| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| Rigosertib sodium - ON01910 sodium | Estybon | Axon 2950
CAS [592542-60-4]
MF C21H24NNaO8SMW 473.47
Purity:
99%
Soluble in water and DMSO
Recently added | | axonmedchem |
| TC Mps1 12 | Axon 2755
CAS [1206170-62-8]
MF C17H20N6OMW 324.38
Purity:
99%
Soluble in DMSO
Description
Potent and selective Mps1 (TTK) kinase inhibitor (IC50 value of 6.4 nM) with good cellular activity, pharmacokinetic properties and efficacy in the A549 lung cancer xenograft model. Additionally, TC Mps1 12 suppressed the growth of hepatocellular carcinoma cells via the accumulation of chromosomal instability.
KEYWORDS: TC Mps1 12 | supplier | Mps1 inhibitor | CAS [1206170-62-8] | Non Selective (Mitotic Spindle Checkpoint) | MPS1 Kinase | Inhibitor | Enzymes | TTK | | axonmedchem |
| Solcitinib - GSK 2586184 | GLPG 0778 | Axon 2539
CAS [1206163-45-2]
MF C22H23N5O2MW 389.45
Purity:
98%
Soluble in DMSO
Description
Selective JAK1 inhibitor originally developed for the treatment of systemic lupus erythematosus, psoriasis and ulcerative colitis.
KEYWORDS: Solcitinib | supplier | JAK1 inhibitor | GSK 2586184 | GLPG 0778 | GSK2586184 | GLPG0778 | CAS [1206163-45-2] | JAK-STAT Pathway | JAK | Inhibitor | Janus kinase | inflammatory | lupus erythematosus | psoriasis | ulcerative colitis | | axonmedchem |
| S3I 201 - NSC 74859 | Axon 2313
CAS [501919-59-1]
MF C16H15NO7SMW 365.36
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent, cellular STAT3 inhibitor that inhibits Stat3·Stat3 complex formation and Stat3 DNA-binding and transcriptional activities (IC50 value 86 µm for in vitro Stat3–Stat3:DNA disruption). S3I 201 inhibits growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3. Additionally, S3I 201 inhibits the expression of the Stat3-regulated genes encoding cyclin D1, Bcl-xL, and survivin and inhibits the growth of human breast tumors in vivo. S3I 201 showed cytotoxic activity against a wide variety of cancer cell lines (IC50 values ranging from 37.9 to 82.6 μm) through inhibition of the reductases P5, protein disulfide isomerase (PDI), thiol-disulfide oxidoreductase ERp57, and/or Trx.
References
Certificates
Categories
Extra info
K. Siddiquee et al. Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proc. Natl. Acad. Sci. USA. 2007, 104, 7391-7396.
S. Fletcher et al. Disruption of transcriptionally active Stat3 dimers with non-phosphorylated, salicylic acid-based small molecules: potent in vitro and tumor cell activities. Chembiochem. 2009, 10, 1959-1964.
T. Horibe et al. Discovery of protein disulfide isomerase P5 inhibitors that reduce the secretion of MICA from cancer cells. Chembiochem. 2014, 15, 1599-1606.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Stem Cell
Transcription Factors
JAK-STAT
TF class 4.2.1
STAT3
Potent, cellular STAT3 inhibitor
Chemical name
2-Hydroxy-4-(2-(tosyloxy)acetamido)benzoic acid
Parent CAS No.
[501919-59-1]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Napabucasin - BBI 608 | FNQ | Axon 2517
CAS [83280-65-3]
MF C14H8O4MW 240.21
Purity:
99%
Soluble in DMSO
Description
Oral first-in-class cancer stemness (CSCs) inhibitor that works by targeting STAT3. Napabucasin is a naturally occurring drug with enhanced toxicity versus glucose-starved tumor cells, and found to induce Mcl-1 cleavage and sustained phosphorylation of c-Jun-N-terminal kinase. Effectively blocks cancer relapse and metastasis in xenografted human cancers.
KEYWORDS: Napabucasin | supplier | STAT3 inhibitor | BBI 608 | FNQ | BBI608 | CAS [83280-65-3] | DNA-RNA | STAT3 | Inhibitor | Transcription Factors | CSCs | cancer stem cell | semness | Mcl-1 | c-Jun-N-terminal kinase | JNK | cancer | | axonmedchem |
| XL 019 | Axon 2231
CAS [945755-56-6]
MF C25H28N6O2MW 444.53
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, selective, and orally active JAK2 inhibitor (IC50 values 2.2 nM and 214.2 nM for JAK2 and JAK3 respectively), showing a significant dose-dependent pharmacodynamic and antitumor effect in a mouse xenograft model. XL 019 significantly inhibits downstream markers pSTAT1 and pSTAT3 (ED50 values 42 mg/kg pSTAT1, and 210 mg/kg pSTAT3).
References
Certificates
Categories
Extra info
S. Verstovsek et al. Phase I evaluation of XL019, an oral, potent, and selective JAK2 inhibitor. Leuk. Res. 2014, 38, 316-322.
T. Forsyth et al. SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg. Med. Chem. Lett. 2012, 22, 7653-7658.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
JAK-STAT
EC 2.7.10.2
JAK
JAK2 inhibitor
Chemical name
(S)-N-(4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)phenyl)pyrrolidine-2-carboxamide
Parent CAS No.
[945755-56-6]
Order
Size
Unit Price
Stock
5 mg
€100.00
In Stock | | axonmedchem |
| Stattic | Axon 2314
CAS [19983-44-9]
MF C8H5NO4SMW 211.19
Purity:
99%
Soluble in DMSO
Description
The first nonpeptidic small-molecule inhibitor of STAT3 activation, dimerization, and nuclear translocation (IC50 value 5.1 μM for inhibition of the binding of a phosphotyrosine-containing peptide derived from the gp130 receptor to the STAT3 SH2 domain). Stattic demonstrates good selectivity for STAT3 inhibition over STAT1, and increases the apoptotic rate of STAT3-dependent breast cancer cell lines.
References
Certificates
Categories
Extra info
H. Chen et al. Discovery of potent anticancer agent HJC0416, an orally bioavailable small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3). Eur. J. Med. Chem. 2014, 82, 195-203.
J. Schust et al. Stattic: a small-molecule inhibitor of STAT3 activation and dimerization. Chem. Biol. 2006, 11, 1235-1242.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Stem Cell
Transcription Factors
JAK-STAT
TF class 4.2.1
STAT3
Nonpeptidic small-molecule inhibitor of STAT3 activation, dimerization, and nuclear translocation
Chemical name
6-nitroBenzo[b]thiophene-1,1-dioxide
Parent CAS No.
[19983-44-9]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| Amcasertib - BBI503 | Axon 2971
CAS [1129403-56-0]
MF C31H33N5O2SMW 539.69
Purity:
98%
Soluble in DMSO
Recently added | | axonmedchem |
| Brassinin | Axon 2489
CAS [105748-59-2]
MF C11H12N2S2MW 236.36
Purity:
98%
Soluble in DMSO
Description
Bioavailable dithiocarbamate with affinity for indoleamine 2,3-dioxygenase (IDO; Ki value 28 μM for human IDO) showing antifungal and anticancer activity. Moreover, Brassinin suppressed both constitutive and IL-6-inducible STAT3 activation through modulation of PIAS-3 and SOCS-3, thereby attenuating tumor growth and increasing sensitivity to paclitaxel.
KEYWORDS: Brassinin | supplier | Dual IDO1/STAT3 inhibitor | CAS [105748-59-2] | L-Kynurenine | IDO1 | STAT3 | Inhibitor | IL-6 | PIAS-3 | SOCS-3 | antifungal | anticancer | natural | dithiocarbamate | paclitaxel | | axonmedchem |
| AS 1517499 | Axon 1992
CAS [919486-40-1]
MF C20H20ClN5O2MW 397.86
Purity:
99%
Soluble in DMSO
Description
Potent and selective STAT6 inhibitor (IC50: 21 nM)
KEYWORDS: AS 1517499 | supplier | STAT6 inhibitor | AS1517499 | AS-1517499 | CAS [919486-40-1] | DNA-RNA | STAT6 | Inhibitor | Transcription Factor | NF-κB | IL-13 | TNF-α | asthma | interleukin | | axonmedchem |
| AT 9283 | Axon 2219
CAS [896466-04-9]
MF C19H23N7O2MW 381.43
Purity:
99%
Soluble in water and DMSO
Description
A multitargeted kinase inhibitor with high affinity for Aurora A and B, JAK2/3, and BCR-Abl(T315I) (IC50 values 3, 3, 1.2, 1.1, and 4 nM respectively). AT 9283 has a potent anti-proliferative activity in a panel of Ba/F3 and human cell lines expressing the BCR-Abl fusion protein or its mutant forms including T315I, and it has the potential to significantly benefit patients with imatinib-resistant CML or with Ph+ ALL.
References
Certificates
Categories
Extra info
W. Qi et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int. J. Cancer. 2012, 130, 2997-3005.
R. Tanaka et al. Activity of the multitargeted kinase inhibitor, AT9283, in imatinib-resistant BCR-ABL-positive leukemic cells. Blood. 2010, 116, 2089-2095.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
Immunology
Pain & Inflammation
BCR-ABL
JAK-STAT
EC 2.7.10.2
Aurora
JAK
Multitargeted kinase inhibitor (Aurora A/B, JAK2/3, and BCR-Abl)
Chemical name
1-cyclopropyl-3-(3-(6-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)urea
Parent CAS No.
[896466-04-9]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Baricitinib - INCB 028050 | LY 3009104 | Axon 1955
CAS [1187594-09-7]
MF C16H17N7O2SMW 371.42
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective and orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (5.9 nM) and JAK2 (5.7 nM); INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM
References
Certificates
Categories
Extra info
JS Fridman et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J. Immunol. 2010, 184(9), 5298-5307.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
Immunology
Pain & Inflammation
JAK-STAT
EC 2.7.10.2
JAK
Inhibitor of JAK1 and JAK2
Chemical name
2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile
Parent CAS No.
[1187594-09-7]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| INCB 024360 - Epacadostat | Axon 1733
CAS [1204669-58-8]
MF C11H13BrFN7O4SMW 438.23
Purity:
98%
Soluble in DMSO
Description
Potent competitive inhibitor of indoleamine 2,3-dioxygenase (IDO1, IC50 value 72 nM in vitro) with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model; INCB024360 (Epacadostat) decreased kynurenine levels by >50% in plasma and inhibited B16-GM-CSF tumor growth in a dose dependent fashion.
An analog of INCB 024360 (Axon 2215) is available as well.
KEYWORDS: INCB 24360 | IDO1 inhibitor | Axon 1733 | Epacadostat | INCB 024360 | INCB024360 | INCB24360 | CAS [1204669-58-8] | [1204669-37-3] | Kynurenine | cancer | immunotherapy | melanoma | hydroxamidine | | axonmedchem |
| JAK2 inhibitor 13 - Sulfonamide 13 | Axon 1843
CAS [1110502-30-1]
MF C17H20N4O2SMW 344.43
Purity:
99%
Soluble in DMSO
Description
Potent and selective Janus Kinase 2 (JAK2) inhibitor; inhibits the activity of both the wild-type JAK2 and the V617F mutant (IC50 = 78 and 206 nM, respectively), with >35-fold selectivity versus JAK3 (IC50 = 2.93 µM)
References
Certificates
Categories
Extra info
S Antonysamy et al. Fragment-based discovery of JAK-2 inhibitors. Bioorg. Med. Chem. Lett. 2009, 19(1), 279-282.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
JAK-STAT
EC 2.7.10.2
JAK
JAK2 inhibitor
Chemical name
4-(3-amino-1H-indazol-5-yl)-N-tert-butylbenzenesulfonamide
Parent CAS No.
[1110502-30-1]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| AZ 960 | Axon 1778
CAS [905586-69-8]
MF C18H16F2N6MW 354.36
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, selective and ATP-competitive JAK2 inhibitor; AZ960 inhibits JAK2 kinase with a Ki of 0.45 nM in vitro and induces growth arrest and apoptosis in adult T-cell leukemia (ATL) cell
References
Certificates
Categories
Extra info
JM Gozgit et al. Effects of the JAK2 Inhibitor, AZ960, on Pim/BAD/BCL-xL Survival Signaling in the Human JAK2 V617F Cell Line SET-2. J. Biol. Chem. 2008, 283(47), 32334-32343.
J Yang et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010, 9(12), 3386-3395.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Epigenetics
JAK-STAT
EC 2.7.10.2
JAK
JAK2 inhibitor
Chemical name
(S)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile
Parent CAS No.
[905586-69-8]
Order
Size
Unit Price
Stock
2 mg
€95.00
In Stock | | axonmedchem |
| UPF 648 | Axon 2118
CAS [213400-34-1]
MF C11H8Cl2O3MW 259.09
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent and selective inhibitor of kynurenine-3-monooxygenase (KMO, or kynurenine hydroxylase) activity (IC50: 20 nM); Active (+)-(1S,2S)-enantiomer; Useful tool for research on cognitive enhancement and neuroprotection in the brain.
References
Certificates
Categories
Extra info
R. Pellicciari et al. Modulation of the kynurenine pathway of tryptophan metabolism in search for neuroprotective agents. Focus on kynurenine-3-hydroxylase. Adv. Exp. Med. Biol. 2003, 527, 621–628.
MT Sapko et al. Endogenous kynurenate controls the vulnerability of striatal neurons to quinolinate: implications for Huntington's disease. Exp. Neurol. 2006, 197(1), 31-40.
L Amori et al. On the relationship between the two branches of the kynurenine pathway in the rat brain in vivo. J. Neurochem. 2009, 109(2), 316-325.
M Amaral et al. Structural basis of kynurenine 3-monooxygenase inhibition. Nature 2013, 496, 382–385.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Pain & Inflammation
KMO
EC 1.14.13.9
Potent inhibitor of kynurenine-3-monooxygenase (KMO)
Chemical name
(1S,2S)-2-(3,4-dichlorobenzoyl)cyclopropanecarboxylic acid
Parent CAS No.
[213400-34-1]
Order
Size
Unit Price
Stock
2 mg
€115.00
In Stock | | axonmedchem |
| CYT 387 - Momelotinib | Axon 1681
CAS [1056634-68-4]
MF C23H22N6O2MW 414.46
Purity:
99%
Soluble in DMSO
Description
Selective and ATP-competitive Janus Kinase JAK1/JAK2 inhibitor, with IC50 to be 11 and 18 nM for JAK1 and JAK2 respectively and far less activity against other kinases, including JAK3 (IC50=155 nM)
References
Certificates
Categories
Extra info
A Pardanan et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia 2009, 23, 1441–1445.
JW Tyner et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 2010, 115(25), 5232-5240.
S Verstovsek. Therapeutic potential of JAK2 inhibitors. Hematology Am Soc Hematol Educ Program. 2009, 636-642.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
JAK-STAT
EC 2.7.10.2
JAK
JAK1 and JAK2 inhibitor
Chemical name
N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide
Parent CAS No.
[1056634-68-4]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| RO 61-8048 | Axon 2139
CAS [199666-03-0]
MF C17H15N3O6S2MW 421.45
Purity:
99%
Soluble in DMSO
Description
Potent, selective and reversible inhibitor of kynurenine-3-monooxygenase (KMO, or kynurenine hydroxylase) activity (IC50: 37 nM); cell-permeable and competitive
References
Certificates
Categories
Extra info
R. Cozzi et al. Kynurenine hydroxylase inhibitors reduce ischaemic brain damage: studies with (m-nitrobenzoyl)alanine and 3,4-dimethoxy-[N-4-(nitrophenyl)thiazol-2-yl]-benzenesulfonamide (...). J. Cereb. Blood Flow Metab., 1999, 19, 771–777.
A. Chiarugi, F. Moroni. Quinolinic acid formation in immuno-activated mice: studies with (m-nitrobenzoyl)-alanine (mNBA) and 3,4-dimethoxy-[N-4-(3-nitrophenyl)thiazol-2-yl[benzenesulphonamide (Ro61-8048), (...). Neuropharmacol. 1999, 38, 1225–1233.
TW Stone. Development and therapeutic potential of kynurenic acid and kynurenine derivatives for neuroprotection. Trends in Pharmacol. Sci. 2000, 21(4), 149–154.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
KMO
EC 1.14.13.9
Inhibitor of kynurenine-3-monooxygenase (KMO)
Chemical name
3,4-dimethoxy-N-(4-(3-nitrophenyl)thiazol-2-yl)benzenesulfonamide
Parent CAS No.
[199666-03-0]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| BFF 122 - BF 5 | Axon 2237
CAS [1152314-49-2]
MF C17H19FN4O4MW 362.36
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective inhibitor of kynurenine aminotransferase II (IC50 values ca. 1 μM and >30 μM for KAT II and KAT I respectively). Intrastriatal BFF 122 decreased newly formed KYNA by 66%, without influencing 3-HK or QUIN production in naïve rats.
References
Certificates
Categories
Extra info
L. Amori et al. On the relationship between the two branches of the kynurenine pathway in the rat brain in vivo. J. Neurochem. 2009, 109, 316-325.
F. Rossi et al. Crystal structure-based selective targeting of the pyridoxal 5'-phosphate dependent enzyme kynurenine aminotransferase II for cognitive enhancement. J. Med. Chem. 2010, 53, 5684-5689.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
KAT II
EC 2.6.1.7
Potent and selective inhibitor of kynurenine aminotransferase II
Chemical name
(S)-10-(4-aminopiperazin-1-yl)-9-fluoro-3-methyl-7-oxo-3,7-dihydro-2H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
Parent CAS No.
[1152314-49-2]
Order
Size
Unit Price
Stock
5 mg
€165.00
In Stock | | axonmedchem |
| INCB 024360-analog - IDO inhibitor 5l | Axon 2215
CAS [914471-09-3]
MF C9H7ClFN5O2MW 271.64
Purity:
99%
Soluble in DMSO
Description
Potent competitive inhibitor of indoleamine 2,3-dioxygenase (IDO1, IC50 value 67 nM) with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model; This INCB024360-analog decreased kynurenine levels by >50% in plasma and inhibited B16-GM-CSF tumor growth in a dose dependent fashion.
INCB 024360 (or Epacadostat; Axon 1733) is available from Axon Medchem as well.
References
Certificates
Categories
Extra info
E.W. Yue et al. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model. J. Med. Chem. 2009, 52, 7364-7367.
X. Liu et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood 2010, 115, 3520-3530.
X. Huang et al. Synthesis of [(18) F] 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide (IDO5L): a novel potential PET probe for imaging of IDO1 expression. J Labelled Comp Radiopharm. 2015 Apr;58(4):156-62.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Immunology
Pain & Inflammation
IDO1
EC 1.13.11.52
Potent inhibitor of indoleamine 2,3-dioxygenase-1 (IDO1)
Chemical name
4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Parent CAS No.
[914471-09-3]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| TG 101348 - Fedratinib | SAR 302503 | Axon 1588
CAS [936091-26-8]
MF C27H36N6O3SMW 524.68
Purity:
99%
Soluble in DMSO
Description
An orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 (JAK2, IC50: ca 3 nM) with potential antineoplastic activity.
KEYWORDS: TG 101348 | supplier | JAK2 inhibitor | Fedratinib | SAR 302503 | TG101348 | SAR302503 | TG-101348 | SAR-302503 | CAS [936091-26-8] | JAK-STAT Pathway | Janus-associated kinase | antineoplastic | hematopoietic stem cell | HSC | | axonmedchem |
| Ruxolitinib - INCB 018424 phosphate | Axon 1598
CAS [1092939-17-7]
MF C17H18N6.H3O4PMW 404.36
Purity:
99%
Optical purity:
98% ee
Soluble in water and DMSO
Description
An orally bioavailable, potent and selective inhibitor of Janus-associated kinase (JAK) 1 and 2, with IC50 to be 2.7, 4.5 and 332 nM for JAK1, JAK2 and JAK3 respectively; selectivity >100 fold for a wide range of other kinases. It acts by blocking the JAK/STAT pathway
References
Certificates
Categories
Extra info
RA Mesa. Ruxolitinib, a selective JAK1 and JAK2 inhibitor for the treatment of myeloproliferative neoplasms and psoriasis. IDrugs. 2010, 13(6), 394-403.
C Campas-Moya. Ruxolitinib. Drugs Fut. 2010, 35(6), 457.
S Verstovsek et al. Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis. N. Engl. J. Med. 2010, 363(12), 1117-1127.
A Quintas-Cardama et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 2010, 115(15), 3109-3117.
E Apostolidou et al. JAK2 inhibitors: a reality? a hope? Clin. Lymp Myel. 2009, 9(Suppl. 3), S340-S345.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
JAK-STAT
EC 2.7.10.2
JAK
JAK1 and JAK2 inhibitor
Chemical name
(R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate
Parent CAS No.
[941678-49-5]
Order
Size
Unit Price
Stock
2 mg
€70.00
In Stock | | axonmedchem |
| AG 490 - Tyrphostin AG 490 | Tyrphostin B42 | Axon 1378
CAS [133550-30-8]
MF C17H14N2O3MW 294.30
Purity:
99%
Soluble in 0.1N NaOH(aq), DMSO, and Ethanol
Description
Janus Kinase 2 (JAK2) inhibitor
References
Certificates
Categories
Extra info
N Miyamoto et al. The JAK2 inhibitor AG490 predominantly abrogates the growth of human B-precursor leukemic cells with 11q23 translocation or Philadelphia chromosome. Leukemia 2001, 15, 1758-1768.
O Sareila et al. JAK Inhibitors AG-490 and WHI-P154 Decrease IFN-γ-Induced iNOS Expression and NO Production in Macrophages. Mediators Inflamm. 2006,2006(2), 16161.
N Meydan, et al. Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor.Nature 1996, 379, 645-648.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Epigenetics
JAK-STAT
EC 2.7.10.2
JAK
JAK2 inhibitor
Chemical name
(E)-N-Benzyl-2-cyano-3-(3,4-dihydro
xy-phenyl)-acrylamide
Parent CAS No.
[133550-30-8]
Order
Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| Gisadenafil besylate - UK 369003 | PF 01224715 | Axon 2218
CAS [334827-98-4]
MF C22H31N7O5S.C7H8O3SMW 677.79
Purity:
99%
Soluble in water and DMSO
Description
Potent and selective inhibitor of cGMP-specific PDE5 (IC50 value 1.23 nM) with improved selectivity over PDE6 (PDE5/6 selectivity value 117 and >3000-fold selectivity over other PDEs). Gisadenafil has the potential for oral bioavailability and dose-proportional pharmacokinetics.
Close analogue of Sildenafil (Viagra; Axon 2046)
References
Certificates
Categories
Extra info
D.J. Rawson et al. The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics. Bioorg. Med. Chem. 2012, 20, 498-509.
N.A.M. Tamimi et al. A placebo-controlled study investigating the efficacy and safety of the phosphodiesterase type 5 inhibitor UK-369,003 for the treatment of men with lower urinary tract symptoms associated (...). BJU Int. 2010, 106, 674–680.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Immunology
EC 3.1.4.35
PDE
Pfizer Licensed Products
Potent and selective inhibitor of PDE5
Chemical name
5-(2-ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)pyridin-3-yl)-3-ethyl-2-(2-methoxyethyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one benzenesulfonate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[334826-98-1]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| Apremilast - CC 10004 | Axon 1957
CAS [608141-41-9]
MF C22H24N2O7SMW 460.50
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Orally active inhibitor of phosphodiesterase-4 (PDE4); an investigational drug for ankylosing spondylitis, psoriasis, and psoriatic arthritis. Apremilast reduces TNF-α production from human synovial cells and significantly suppresses experimental arthritis
References
Certificates
Categories
Extra info
K Papp et al. Efficacy of apremilast in the treatment of moderate to severe psoriasis: a randomised controlled trial. Lancet, 2012, 380 (9843), 738-746.
P Schafer. Apremilast mechanism of action and application to psoriasis and psoriatic arthritis. Biochem. Pharmacol. 2012, 83 (12), 1583–1590.
FE McCann et al. Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis. Arthritis Res. Ther. 2010, 12(3), R107.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Immunology
Pain & Inflammation
EC 3.1.4.53
PDE
PDE4 inhibitor
Chemical name
(S)-N-(2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-1,3-dioxoisoindolin-4-yl)acetamide
Parent CAS No.
[608141-41-9]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| PF 04859989 hydrochloride - L-3-Amino-3,4-dihydro-1-hydroxycarbstyril hydrochloride | Axon 2924
CAS [177943-33-8]
MF C9H10N2O2.HClMW 214.65
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Recently added | | axonmedchem |
| Sildenafil citrate - Viagra | UK 92480 | Axon 2046
CAS [171599-83-0]
MF C22H30N6O4S.C6H8O7MW 666.70
Purity:
100%
Soluble in DMSO
Description
Potent and selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) with IC50 value of 4 nM; Enhances nitric oxide (NO)-dependent relaxation of human corpus cavernosum in vitro; an oral therapy for erectile dysfunction (ED)
References
Certificates
Categories
Extra info
M Boolell et al. Sildenafil: an orally active type 5 cyclic GMP-specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. Int. J. Impot. Res. 1996, 8 (2), 47–52.
I Goldstein et al. Oral Sildenafil in the Treatment of Erectile Dysfunction. N. Engl. J. Med. 1998, 338, 1397-1404.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
EC 3.1.4.35
PDE
Pfizer Licensed Products
Inhibitor of cGMP-specific PDE5
Chemical name
5-(2-ethoxy-5-(4-methylpiperazin-1-ylsulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one 2-hydroxypropane-1,2,3-tricarboxylate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[139755-83-2]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Rolipram, (S)-(+)- | Axon 1432
CAS [85416-73-5]
MF C16H21NO3MW 275.34
Purity:
99%
Soluble in DMSO and Ethanol
Description
PDE4 inhibitor, less active S-enantiomer of Rolipram (Axon 1212) in comparison with the opposite (R)-(-)-Rolipram (Axon 1229)
References
Certificates
Categories
Extra info
HH Schneider et al. Stereospecific binding of the antidepressant rolipram to brain protein structures. Eur. J. Pharmacol. 1986, 127(1-2), 105-15.
DE Griswold et al. Effect of selective phosphodiesterase type IV inhibitor, rolipram, on fluid and cellular phases of inflammatory response. Inflammation. 1993, 17(3), 333–44.
SJ Kanes et al. Rolipram: A specific phosphodiesterase 4 inhibitor with potential antipsychotic activity. Neuroscience. 2006, 144, 239-46.
RW Chen et al. Broad spectrum neuroprotection profile of phosphodiesterase inhibitors as related to modulation of cell-cycle elements and caspase-3 activation. Neuroscience Letters. 2007, 418(2), 165–9.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Pain & Inflammation
EC 3.1.4.53
PDE
PDE4 inhibitor
Chemical name
(4S)-4-[3-(Cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one
Parent CAS No.
[85416-73-5]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| Zardaverine | Axon 1216
CAS [101975-10-4]
MF C12H10F2N2O3MW 268.22
Purity:
99%
Soluble in DMSO
Description
Selective phosphodiesterase III/IV inhibitor (PDE3/4)
References
Certificates
Categories
Extra info
DC Underwood et al. Comparison of phosphodiesterase III, IV and dual III/IV inhibitors on bronchospasm and pulmonary eosinophil influx in guinea pigs. J. Pharmacol. Exp. Ther. 1994, 270, 250.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
EC 3.1.4.17
PDE
PDE3 and PDE4 inhibitor
Chemical name
6-(4-Difluoromethoxy-3-methoxy-phenyl)-2H-pyridazin-3-one
Parent CAS No.
[101975-10-4]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| PDE5 inhibitor 42 | Axon 1709
CAS [936449-28-4]
MF C23H31N7O3MW 453.54
Purity:
98%
Soluble in DMSO
Description
Potent and selective phosphodiesterase type 5 (PDE5) inhibitor (IC50: 0.04 nM); PDE6/PDE5 and PDE11/PDE5 ratios to be 100x and 530x respectively; a second generation PDE5 inhibitor under investigation
References
Certificates
Categories
Extra info
MB Tollefson et al. 1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. Bioorg. Med. Chem. Lett. 2010, 20(10), 3120-3124.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
EC 3.1.4.35
PDE
PDE5 inhibitor
Chemical name
1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H-pyrazolo[4,3-d]pyrimidin-5-yl)piperidine-4-carboxylic acid
Parent CAS No.
[936449-28-4]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| BAY 19-8004 - Lirimilast | Axon 1178
CAS [329306-27-6]
MF C17H12Cl2N2O6SMW 443.26
Purity:
98%
Soluble in DMSO
Description
Selective inhibitor of phosphodiesterase-4 (PDE4)
References
Certificates
Categories
Extra info
D.C. Grootendorst et al. Efficacy of the novel phosphodiesterase-4 inhibitor BAY 19-8004 on lung function and airway inflammation in asthma and chronic obstructive pulmonary disease (COPD). Pulmonary Pharmacol. Ther. 16 (2003) 341–347.
P. Norman. PDE4 inhibitors: sustained patenting activity as leading drugs near the market. Exp. Opin. Ther. Pat.2000, 10, 9, 1415-1427.
D.C. Grootendorst, K.F. Rabe. Selective phosphodiesterase inhibitors for the treatment of asthma and chronic obstructive pulmonary disease. Curr. Opin. Allergy Clin. Immunol. 2002, 2(1), 61-67.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Pain & Inflammation
EC 3.1.4.53
PDE
PDE4 inhibitor
Chemical name
Methanesulfonic acid 2-(2,4-dichloro-benzoyl)-3-ureido-benzofuran-6-yl ester
Parent CAS No.
[329306-27-6]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| Rolipram | Axon 1212
CAS [61413-54-5]
MF C16H21NO3MW 275.34
Purity:
98%
Soluble in DMSO and Ethanol
Description
PDE4 inhibitor, as an anti-inflammatory drug; also with rich CNS profile, such as antidepressive, antipsychotic effects and/or neuroprotection.
KEYWORDS: Rolipram | supplier | PDE4 inhibitor | CAS [61413-54-5] | cAMP | PDE | phosphodiesterase | anti-inflammatory | CNS | anti-depressive | anti-psychotic | neuroprotection | | axonmedchem |
| L 454560 | Axon 1127
CAS [346629-30-9]
MF C31H29N3O5S2MW 587.71
Purity:
98%
Soluble in DMSO
Description
Potent and selective PDE4 inhibitor
References
Certificates
Categories
Extra info
Z Huang et al. L-454,560, a potent and selective PDE4 inhibitor with in vivoefficacy in animal models of asthma and cognition. Biochem. Pharmacol. 2007, 73(12), 1971-1981.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Pain & Inflammation
EC 3.1.4.53
PDE
PDE4 inhibitor
Chemical name
6-(1-Methanesulfonyl-1-methyl-ethyl)-8-{3-[(E)-2-(4-methanesulfonyl-phenyl)-2-(3-methyl-[1,2,4]oxadiazol-5-yl)-vinyl]-phenyl}-quinoline
Parent CAS No.
[346629-30-9]
Order
Size
Unit Price
Stock
5 mg
€165.00
In Stock | | axonmedchem |
| UK 432097 | Axon 1193
CAS [380221-63-6]
MF C40H47N11O6MW 777.87
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective A2A-adenosine receptor agonist; agent developed by Pfizer for chronic obstructive pulmonary disease (category Allergy/Respiratory); its high selectivity has made it useful for detailed mapping of the internal structure of the A2A receptor.
Expert recommendation - a highly recommended tool in research of A2A receptor.
References
Certificates
Categories
Extra info
C. Russo et al. Adenosine receptors: promising targets for the development of novel therapeutics and diagnostics for asthma. Fundam. Clin. Pharmacol. 2006, 20, 9-19.
Safety and efficacy of UK-432,097 in chronic obstructive pulmonary disease. ClinicalTrials.gov 2013.
F. Xu et al. Structure of an Agonist-Bound Human A2A Adenosine Receptor. Science 2011, 332(6027), 322-327.
(* UK 432097 used in this study was procured from Axon Medchem.) | | axonmedchem |
| Aminotetraline hydrochloride, N-Cyclopropyl-2- | Axon 1067
CAS [1246094-94-9]
MF C13H17N.HClMW 223.74
Purity:
98%
Soluble in water
Description
MAO inhibitor
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
CNS
MAO
EC 1.4.3.4
MAO inhibitor
Chemical name
Cyclopropyl-(1,2,3,4-tetrahydro-naphthalen-2-yl)-amine hydrochloride
Parent CAS No.
[1152892-99-3]
Inquire | | axonmedchem |
| Aminotetraline hydrobromide, N-Cyclopropyl-N-methyl-2- - CMAT | Axon 1066
CAS [1246094-80-3]
MF C14H19N.HBrMW 282.22
Purity:
99%
Soluble in water
Description
MAO inhibitor
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
CNS
MAO
EC 1.4.3.4
MAO inhibitor
Chemical name
Cyclopropyl-methyl-(1,2,3,4-tetrahydro-naphthalen-2-yl)-amine hydrobromide
Parent CAS No.
[1246242-28-3]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| SCH 442416, Desmethyl | Axon 2283
CAS [188112-92-7]
MF C19H17N7O2MW 375.38
Purity:
95%
Soluble in DMSO
Description
Precursor for [11C]SCH442416 for PET studies; Radioligand precursor of the highly selective and potent A2A adenosine receptor antagonist SCH 442416 (Axon 1264). Desmethyl SCH 442416 is less potent and less selective in binding the A2A receptor than SCH 445416 (Ki values 44 nM, 48 nM, and 34 nM for A1, A2A and A3 respectively).
References
Certificates
Categories
Extra info
K. Ishiwata et al. PET Tracers for mapping adenosine receptors as probes for diagnosis of CNS disorders. CNS Agents Med. Chem. 2007, 7, 55-57.
Toddle et al. Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A2A receptor system using positron emission tomography. J. Med. Chem. 2000, 43, 4359.
A.K. Bhattacharjee et al. Striatal adenosine A2A receptor mediated PET Imaging in 6-hydroxydopamine lesioned rats using [18F]-MRS5425. Nucl. Med. Biol. 2011, 38, 897-906.
B.A. Shinkre et al. Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. Bioorg. Med. Chem. Lett. 2010, 20, 5690-5694.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
A1
A2A
A3
A18
Non Selective
Radioligand precursor of the adenosine A2A antagonist SCH 442416
Chemical name
4-(3-(5-amino-2-(furan-2-yl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-7-yl)propyl)phenol
Parent CAS No.
[188112-92-7]
Order
Size
Unit Price
Stock
10 mg
€300.00
In Stock | | axonmedchem |
| MRS 1523 | Axon 2076
CAS [212329-37-8]
MF C23H29NO3SMW 399.55
Purity:
98%
Soluble in DMSO
Description
Potent and highly selective adenosine A3 receptor antagonist (Ki= 18.9 nM for human A3R)
References
Certificates
Categories
Extra info
B Shimpukade et al. Discovery of a Potent and Selective GPR120 Agonist. J. Med. Chem. 2012, 55 (9), 4511–4515.
BD Hudson et al. Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids. Mol. Endocrinol. 2013, doi:10.1210/me.2013-1085.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
A3
A18
Adenosine A3 receptor antagonist
Chemical name
propyl 6-ethyl-5-(ethylthiocarbonyl)-2-phenyl-4-propylnicotinate
Parent CAS No.
[212329-37-8]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| BAY 60-6583 - BR 4887 | Axon 2317
CAS [910487-58-0]
MF C19H17N5O2SMW 379.44
Purity:
99%
Soluble in DMSO
Description
Potent and highly selective A2BAR (Adenosine) agonist (Ki value 0.33-0.75 nM, species dependent). BAY 60-6583 potently stimulated cAMP production in HEK 293 cells expressing mouse A2BARs (EC50 value 2.83 nM), and BAY 60-6583 produced a biphasic effect on fMLP-stimulated superoxide production.
References
Certificates
Categories
Extra info
J.A. Auchampach et al. Characterization of the A2B adenosine receptor from mouse, rabbit, and dog. J Pharmacol Exp Ther. 2009 Apr;329(1):2-13.
D. van der Hoeven et al. A role for the low-affinity A2B adenosine receptor in regulating superoxide generation by murine neutrophils. J Pharmacol Exp Ther. 2011 Sep;338(3):1004-12.
S. Hinz et al. BAY60-6583 acts as a partial agonist at adenosine A2B receptors. J Pharmacol Exp Ther. 2014 Jun;349(3):427-36.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
A18
A2B
Potent and highly selective A2BAR (Adenosine) agonist
Chemical name
2-(6-amino-3,5-dicyano-4-(4-(cyclopropylmethoxy)phenyl)pyridin-2-ylthio)acetamide
Parent CAS No.
[910487-58-0]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Rolofylline metabolite M1-cis - Compound 4 | Axon 1852
CAS [161167-65-3]
MF C20H28N4O3MW 372.46
Purity:
98%
Soluble in DMSO and Ethanol
Description
Active metabolite of Rolofylline (Axon 1603), a potent and selective adenosine A1 receptor antagonist
References
Certificates
Categories
Extra info
W Radziszewski et al. A single supratherapeutic dose of rolofylline does not prolong the QTcF interval in healthy volunteers. Am. J. Ther. 2010, 17(1), 8-16.
M Stroh et al. The Effects of Multiple Doses of Rolofylline on the Single-Dose Pharmacokinetics of Midazolam in Healthy Subjects. Am. J. Ther. 2010, 17(1), 53-60.
Certificate of Analysis
Material Safety Data Sheet
CNS
A1
A18
Adenosine A1 antagonist
Chemical name
8-(Hexahydro-7-hydroxy-2,5-methanopentalen-3a(1H)-yl)-3,9-dihydro-1,3-dipropyl-1H-Purine-2,6-dione, cis
Parent CAS No.
[161167-65-3]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| ABT 702 | Axon 2289
CAS [214697-26-4]
MF C22H19BrN6OMW 463.33
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
The first, non-nucleoside adenosine kinase (ADK) inhibitor (IC50 value 2 nM and 50 nM in cytosolic and intact cell assays, respectively). ABT702 is orally active to reduce pain and inflammation in animal models, yet found to be clastogenic in an in vitro Chinese Hamster micronucleus assay.
KEYWORDS: ABT 702 | supplier | ADK inhibitor | ABT702 | CAS [214697-26-4] | ATP | ADK | pain | inflammation | clastogenic | mutagenesis | | axonmedchem |
| KW 6002 - Istradefylline | Axon 1423
CAS [155270-99-8]
MF C20H24N4O4MW 384.43
Purity:
99%
Soluble in DMSO
Description
Very potent, selective and orally active adenosine A2A receptor antagonist in experimental models of Parkinson's disease
References
Certificates
Categories
Extra info
S Shiozaki et al. Actions of adenosine A2A receptor antagonist KW-6002 on drug-induced catalepsy and hypokinesia caused by reserpine or MPTP. Psychopharmacology (Berl). 1999, 147(1), 90-95.
TN Chase et al. Translating A2A antagonist KW6002 from animal models to parkinsonian patients. Neurology 2003, 61(11 Suppl 6), S107-11.
PA LeWitt et al. Adenosine A2A receptor antagonist istradefylline (KW-6002) reduces "off" time in Parkinson's disease: a double-blind, randomized, multicenter clinical trial (6002-US-005). Ann. Neurol. 2008, 63(3), 295-302.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
A2A
A18
Adenosine A2A antagonist
Chemical name
8-[(E)-2-(3,4-Dimethoxy-phenyl)-vinyl]-1,3-diethyl-7-methyl-3,7-dihydro-purine-2,6-dione
Parent CAS No.
[155270-99-8]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Rolofylline metabolite M1-trans - Compound 3 | Axon 1851
CAS [160943-06-6]
MF C20H28N4O3MW 372.46
Purity:
99%
Soluble in DMSO
Description
Active metabolite of Rolofylline (Axon 1603), a potent and selective adenosine A1 receptor antagonist
References
Certificates
Categories
Extra info
W Radziszewski et al. A single supratherapeutic dose of rolofylline does not prolong the QTcF interval in healthy volunteers. Am. J. Ther. 2010, 17(1), 8-16.
M Stroh et al. The Effects of Multiple Doses of Rolofylline on the Single-Dose Pharmacokinetics of Midazolam in Healthy Subjects. Am. J. Ther. 2010, 17(1), 53-60.
Certificate of Analysis
Material Safety Data Sheet
CNS
A1
A18
Adenosine A1 antagonist
Chemical name
8-(Hexahydro-7-hydroxy-2,5-methanopentalen-3a(1H)-yl)-3,9-dihydro-1,3-dipropyl-1H-Purine-2,6-dione, trans
Parent CAS No.
[160943-06-6]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| CGS 21680 hydrochloride | Axon 1319
CAS [124431-80-7]
MF C23H29N7O6.HClMW 535.98
Purity:
98%
Soluble in DMSO
Description
Selective A2A adenosine receptor agonist.
KEYWORDS: CGS 21680 hydrochloride | supplier | 124431-80-7 | 120225-54-9 | 124182-57-6 | Axon 1319 | A2A agonist | CGS21680 | CGS21680 | A2A | adenosine | | axonmedchem |
| GR 79236 | Axon 1287
CAS [124555-18-6]
MF C15H21N5O5MW 351.36
Purity:
99%
Soluble in water, DMSO and Ethanol
Description
Adenosine A1 receptor agonist
References
Certificates
Categories
Extra info
Merkel et al. Cardiovascular and antilipolytic effects of the adenosine agonist GR 79236. Pharmacology 1995, 51, 224.
LJ Knutsen et al. N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J. Med. Chem. 1999, 42, 3463-3477.
Thompson, C. et al. Triacylglycerol lowering properties of the adenosine analog GR 79236 during 5 days of dosing large, old rats: A pilot study Nutrition Res. 1996, 1925-1932.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
A1
A18
Adenosine A1 agonist
Chemical name
(2R,3S,5R)-2-[6-((1S,2S)-2-Hydroxy-cyclopentylamino)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol
Parent CAS No.
[124555-18-6]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| Deazaadenosine, 1- | Axon 2434
CAS [14432-09-8]
MF C11H14N4O4MW 266.25
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Inhibitor of adenosine deaminase (ADA; IC50 value 0.38 μM) 1-Deazaadenosine showed cytostatic activity against multiple cell lines in vitro.
KEYWORDS: 1-Deazaadenosine | supplier | ADA inhibitor | CAS [14432-09-8] | Adenosine | deaminase | cytostatic | antitumor | | axonmedchem |
| SDZ-WAG 994 - WAG 994 | N-Cyclohexyl-2'-O-methyladenosine | Axon 1265
CAS [130714-47-5]
MF C17H25N5O4MW 363.41
Purity:
98%
Soluble in DMSO and Ethanol
Description
Potent, selective and orally active A1 adenosine receptor agonist.
KEYWORDS: SDZ-WAG 994 | supplier | A1 agonist | WAG 994 | N-Cyclohexyl-2'-O-methyladenosine | SDZ-WAG994 | WAG994 | WAG-994 | CAS [130714-47-5] | Adenosine | A1 | Agonist | Receptors | | axonmedchem |
| Trelagliptin succinate - SYR 111472 succinate | SYR 472 | Axon 2470
CAS [1029877-94-8]
MF C18H20FN5O2.C4H6O4MW 475.47
Purity:
100%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Orally active DPP-4 inhibitor that produces clinically and statistically significant improvements in glycaemic control in patients with type 2 diabetes. SYR472 has a long duration of action and is well tolerated in clinical studies.
References
Certificates
Categories
Extra info
N. Inagaki et al. SYR-472, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet Diabetes Endocrinol. 2014 Feb;2(2):125-32.
K. V. T. S. Pavan Kumar et al. Study of plant glucosylxanthone & its analogs, as DPPIV inhibitor for anti-diabetic activity. Int. J. Pharm. Sci. Rev. Res., 15(1), 2012, 17, 83-87.
A.J. Garber et al. The importance of incretin therapies for managing type 2 diabetes. Lancet Diabetes Endocrinol. 2014 Feb;2(2):95-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
DPP4
EC 3.4.14.5
Orally active DPP4 inhibitor for the treatment of type 2 diabetes
Chemical name
(R)-2-((6-(3-aminopiperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile succinate
Parent CAS No.
[865759-25-7]
Order
Size
Unit Price
Stock
10 mg
€145.00
In Stock | | axonmedchem |
| SCH 442416 | Axon 1264
CAS [316173-57-6]
MF C20H19N7O2MW 389.41
Purity:
99%
Soluble in DMSO
Description
Highly selective and potent A2A adenosine receptor antagonist.
The desmethyl derivative of SCH 442416 (Axon 2283) is a valuable precursor for [11C]SCH442416 PET studies, and is available from Axon Medchem as well.
KEYWORDS: SCH 442416 | supplier | A2A antagonist | SCH442416 | CAS [316173-57-6] | Adenosine | A2A | Antagonist | neurodegenerative | Parkinson’s |Huntington’s | PET | positron | nucleoside | PD | HD | movement disorder | | axonmedchem |
| Butabindide oxalate | Axon 1228
CAS [185213-03-0]
MF C17H25N3O2.C2H2O4MW 393.43
Purity:
99%
Optical purity:
Optically pure
Soluble in water
Description
Inhibitor of tripeptidyl peptidase II (TPPII)
References
Certificates
Categories
Extra info
C. Robin Ganellin et al. Inhibitors of Tripeptidyl Peptidase II. 3. Derivation of Butabindide by Successive Structure Optimizations Leading to a Potential General Approach to Designing Exopeptidase Inhibitors. J. Med. Chem. 2005, 48 (23), 7333-7342.
AJ Book et al. Tripeptidyl Peptidase II. An Oligomeric Protease Complex from Arabidopsis. Plant Physiol. 2005, 138(2), 1046–1057.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
TPP2
EC 3.4.14.10
TPP2 inhibitor
Chemical name
(S)-1-((S)-2-Amino-butyryl)-2,3-dihydro-1H-indole-2-carboxylic acid butylamide oxalate
Parent CAS No.
[175553-48-7]
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10 mg
€105.00
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