| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| PFM01 | Axon 2821
CAS [1558598-41-6]
MF C14H15NO2S2MW 293.40
Purity:
99%
Soluble in DMSO
Description
PFM01 is an inhibitor of MRE11 endonuclease which forms the core of the MRE11-RAD50-NBS1 (MRN) complex. The MRN complex has essential roles in detecting, signaling, protecting and repairing DNA double strand breaks.
KEYWORDS: PFM01 | supplier | Endonuclease inhibitor | PFM 01 | PFM-01 | CAS [1558598-41-6] | DNA-RNA | Endonuclease | Inhibitor | Enzymes | MRE11 | MRN complex | | axonmedchem |
| CNF 2024 - BIIB 021 | Axon 1543
CAS [848695-25-0]
MF C14H15ClN6OMW 318.76
Purity:
99%
Soluble in DMSO
Description
Oral inhibitor of heat shock protein 90 (Hsp90) under clinical development
References
Certificates
Categories
Extra info
B Böll et al. Heat Shock Protein 90 Inhibitor BIIB021 (CNF2024) Depletes NF-κB and Sensitizes Hodgkin's Lymphoma Cells for Natural Killer Cell–Mediated Cytotoxicity. Clin. Cancer Res. 2009, 15(16), 5108–16.
T Taldone et al. Targeting Hsp90: small-molecule inhibitors and their clinical development. Cur. Opin. Pharmacol. 2008, 8(4), 370-374.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
Hsp90
EC 3.6
Hsp90 inhibitor
Chemical name
6-Chloro-9-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-9H-purin-2-ylamine
Parent CAS No.
[848695-25-0]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| NVP-AUY922 - VER 52296 | Luminespib | Axon 1542
CAS [747412-49-3]
MF C26H31N3O5MW 465.54
Purity:
98%
Soluble in DMSO
Description
Highly potent and oral inhibitor of heat shock protein 90 (Hsp90) in vitro and in vivo, with IC50=21 nM in Hsp90 FP binding assay; inhibits proliferation of various human cancer cell lines in vitro, with GI50 average 9 nM
References
Certificates
Categories
Extra info
MR Jensen et al. NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models. Breast Cancer Res. 2008, 10, R33.
SA Eccles et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Res. 2008, 68, 2850.
PA Brough et al. 4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer. J. Med. Chem., 2008, 51 (2), pp 196–218.
T Taldone et al. Targeting Hsp90: small-molecule inhibitors and their clinical development. Cur. Opin. Pharmacol. 2008, 8(4), 370-374.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
Hsp90
EC 3.6
Hsp90 inhibitor
Chemical name
5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide
Parent CAS No.
[747412-49-3]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| APE1 Inhibitor III | Axon 2137
CAS [524708-03-0]
MF C19H21N3OS2MW 371.52
Purity:
99%
Soluble in DMSO
Description
Cell permeable and competitive inhibitor of apurinic/apyrimidinic (AP) endonuclease 1 (Ape1) activity, exhibiting 2.0 micromolar activity against the purified APE1 enzyme
References
Certificates
Categories
Extra info
G Rai et al. Synthesis, biological evaluation, and structure-activity relationships of a novel class of apurinic/apyrimidinic endonuclease 1 inhibitors. J. Med. Chem. 2012, 55(7), 3101-3112.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
APE1
EC 4.2.99.18
Endonuclease
Inhibitor of apurinic/apyrimidinic endonuclease 1 (APE1)
Chemical name
N-(3-(benzo[d]thiazol-2-yl)-6-isopropyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl)acetamide
Parent CAS No.
[524708-03-0]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| AR03 | Axon 2136
CAS [510721-85-4]
MF C15H15N3MW 237.30
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Specific inhibitor of apurinic/apyrimidinic (AP) endonuclease 1 (Ape1) activity
References
Certificates
Categories
Extra info
A Bapat et al. Novel small-molecule inhibitor of apurinic/apyrimidinic endonuclease 1 blocks proliferation and reduces viability of glioblastoma cells. J. Pharmacol. Exp. Ther. 2010, 334(3), 988-998.
DM Wilson III & A Simeonov. Small molecule inhibitors of DNA repair nuclease activities of APE1. Cell. Mol. Life Sci., 2010, 67(21), 3621-3631.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
APE1
EC 4.2.99.18
Endonuclease
Inhibitor of apurinic/apyrimidinic endonuclease 1 (APE1)
Chemical name
2,4,9-trimethylbenzo[b][1,8]naphthyridin-5-amine
Parent CAS No.
[510721-85-4]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| Hydroxypioglitazone - M-IV | Axon 2533
CAS [146062-46-6]
MF C19H20N2O4S.HClMW 408.90
Purity:
100%
Soluble in DMSO
Description
Active metabolite of Pioglitazone (M-IV), a PPARγ agonist used for the treatment of diabetes mellitus type 2. Showed modest antihyperglycemic activity compared to Pioglitazone. Moreover, Hydroxypioglitazone is more efficient than Pioglitazone in stimulating lipid synthesis at a 3 µM dose in a 3T3-L1 cell assay.
KEYWORDS : Hydroxypioglitazone | supplier | PPARγ agonist | M-IV | CAS [146062-46-6] | [146062-44-4] | Prostaglandins | PPAR | Agonist | diabetes mellitus | type 2 | antihyperglycemic | Pioglitazone | metabolite | | axonmedchem |
| TBOA ammonia salt, L- - TBOA | (3S)-3-(Phenylmethoxy)-L-aspartic acid ammonia salt | Axon 2427
CAS [N.A.]
MF C11H13NO5.NH3MW 256.26
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Very potent blocker for the human excitatory amino acid transporters (EAAT1–3; IC50 values 23 µM, 3.8 µM, 7.0 µM for EAAT1, EAAT2, and EAAT3, respectively). L-TBOA is the most active isomer of DL-TBOA, as sold by competitors, and approximately twice as potent for inhibition of EAAT1 and EAAT2. | | axonmedchem |
| Rosiglitazone - BRL 49653 | Rezult | Rosiglizole | TDZ 01 | Axon 2443
CAS [122320-73-4]
MF C18H19N3O3SMW 357.43
Purity:
98%
Soluble in DMSO
Description
High affinity PPARγ agonist (Kd value 7 nM). BRL 49653 is an antidiabetic drug and insulin sensitizer that also promotes differentiation of C3H10T1/2 stem cells to adipocytes.
References
Certificates
Categories
Extra info
Y.F. Zhang et al. Rosiglitazone, a Peroxisome Proliferator-Activated Receptor (PPAR)-γ Agonist, Attenuates Inflammation Via NF-κB Inhibition in Lipopolysaccharide-Induced Peritonitis. Inflammation. 2015 Jun 6.
J.M. Lehmann et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6.
R.T. Nolte et al. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma. Nature. 1998 Sep 10;395(6698):137-43.
J.C. de Groot et al. Structural characterization of amorfrutins bound to the peroxisome proliferator-activated receptor γ. J Med Chem. 2013 Feb 28;56(4):1535-43.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Diabetes & Metabolism
Pain & Inflammation
NF-κB
PPAR
NR1C
PPARγ agonist; antidiabetic drug and stem cell differentiator
Chemical name
5-(4-(2-(methyl(pyridin-2-yl)amino)ethoxy)benzyl)thiazolidine-2,4-dione
Parent CAS No.
[122320-73-4]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| A 841720 | Axon 2155
CAS [869802-58-4]
MF C17H21N5OSMW 343.45
Purity:
99%
Soluble in DMSO
Description
Potent and selective non-competitive mGlu1 receptor antagonist (IC50: 10 nM); showing 34-fold selectivity over mGluR5 and no significant activity at other mGluR receptors, neurotransmitter receptors, ion channels, and transporters. A 841720 demonstrated full efficacy in various in vivo animal pain models.
KEYWORDS: A 841720 | supplier | mGluR1 antagonist | A841720 | A-841720 | CAS [869802-58-4] | Metabotropic | Glutamate | mGluR1 | mGlu1 | Antagonist | Receptors | | axonmedchem |
| CMPDA | Axon 2079
CAS [380607-77-2]
MF C16H28N2O4S2MW 376.53
Purity:
99%
Soluble in DMSO
Description
Positive allosteric modulator (PAM) of AMPA receptor; more specifically, CMPDA allosterically modulates AMPA subunit GluA2 receptor (GluR2) and its desensitization and deactivation
References
Certificates
Categories
Extra info
DE Timm et al. Structural and functional analysis of two new positive allosteric modulators of GluA2 desensitization and deactivation. Mol. Pharmacol. 2011, 80(2), 267-280.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
AMPA
Unclassified
Positive allosteric modulator of AMPA receptor
Chemical name
N,N'-(2,2'-(1,4-phenylene)bis(ethane-2,1-diyl))dipropane-2-sulfonamide
Parent CAS No.
[380607-77-2]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| ADX71743 | Axon 2732
CAS [N.A.]
MF C17H19NO2MW 269.34
Purity:
99%
Soluble in DMSO
Description
ADX71743 is a selective mGluR7 negative allosteric modulator.
KEYWORDS: ADX71743 | supplier | mGLuR7 NAM | ADX71743 | ADX-71743 | ADX 71743 | Glutamate | mGluR7 | NAM | Receptors | | axonmedchem |
| JNJ 55511118 | Axon 2793
CAS [2036081-86-2]
MF C14H8ClF3N2O2MW 328.67
Purity:
98%
Soluble in DMSO
Description
Potent negative modulator of AMPA receptor containing TARP-γ8 (Ki value of 26 nM). JNJ 55511118 exhibits excellent pharmacokinetic properties and achieved high receptor occupancy following oral administration. Tool for reversible AMPA receptor inhibition, particularly within the hippocampus, with potential therapeutic utility as an anticonvulsant or neuroprotectant.
KEYWORDS: JNJ 55511118 | supplier | AMPA negative modulator | JNJ-55511118 | JNJ55511118 | CAS [2036081-86-2] | Glutamate | AMPA | Negative modulator | Ion Channels | TARP-γ8 | Neuroprotectant | | axonmedchem |
| ZD 9379 | Axon 2261
CAS [170142-20-8]
MF C19H14ClN3O4MW 383.79
Purity:
100%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Selective antagonist of the glycine site on the NMDA receptor complex. ZD9379 crosses the blood-brain barrier and is neuroprotective. In vivo studies demonstrated reduced infarct size and less spreading depressions after treatment with ZD 9379.
References
Certificates
Categories
Extra info
T.M. Bare et al. Pyridazino[4,5-b]quinolinediones: novel glycine/N-methyl-D-aspartate antagonists for the treatment of stroke. J. Heterocyclic Chem. 1998, 35, 1171-1186.
T. Tatlisumak et al. A glycine site antagonist ZD9379 reduces number of spreading depressions and infarct size in rats with permanent middle cerebral artery occlusion. Acta Neurochir. Suppl. 2000, 76, 331-333.
K. Takano et al. Glycine site antagonist attenuates infarct size in experimental focal ischemia. Postmortem and diffusion mapping studies. Stroke. 1997, 28, 1255-1262.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
NMDA
Unclassified
Antagonist of the glycine site on the NMDA receptor complex
Chemical name
7-chloro-2-(4-methoxy-2-methylphenyl)-2,3-dihydropyridazino[4,5-b]quinoline-1,4,10(5H)-trione
Parent CAS No.
[170142-20-8]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| CP 101606 - Traxoprodil | Axon 2254
CAS [134234-12-1]
MF C20H25NO3MW 327.42
Purity:
99%
Optical purity:
98% d.e.
Soluble in water and DMSO
Description
Potent and NR2B selective antagonist of NMDA glutamate receptors.
A water soluble form, CP 101606 mesylate (Axon 1406) is readily available as well.
References
Certificates
Categories
Extra info
K Taniguchi et al. Antinociceptive activity of CP-101,606, an NMDA receptor NR2B subunit antagonist. Br. J. Pharmacol. 1997, 122, 809–812.
FS. Menniti et al. CP-101,606: An NR2B-Selective NMDA Receptor Antagonist. CNS Drug Rev. 1998, 4(4), 307-322.
L. Yurkewicz et al. The effect of the selective NMDA receptor antagonist traxoprodil in the treatment of traumatic brain injury. J. Neurotrauma. 2005, 22(12), 1428-43.
JG Nutt et al. Effects of a NR2B selective NMDA glutamate antagonist, CP-101,606, on dyskinesia and parkinsonist. Mov. Disord. 2008, 23(13), 1860-1866.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
NMDA
Unclassified
NMDA NR2B antagonist
Chemical name
1-[(1S,2S)-2-Hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]-4-phenylpiperidin-4-ol
Parent CAS No.
[134234-12-1]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| TCN-201 | Axon 2708
CAS [852918-02-6]
MF C21H17ClFN3O4SMW 461.89
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
NMDA receptor antagonist selective for NR2A- over NR2B-containing receptors (pIC50 values of 6.8 and 4.3, respectively). The degree of inhibition produced by TCN 201 is dependent on the concentration of the GluN1-site co-agonist, glycine (or D-serine), and is independent of the glutamate concentration. TCN-201 is a negative allosteric modulator of glycine binding.
KEYWORDS: TCN-201 | supplier | NR2A antagonist | TCN201 | TCN 201 | CAS [852918-02-6] | Axon Medchem | Axon 2708 | Glutamate | NMDA | Antagonist | Ion Channels | | axonmedchem |
| RO 25-6981 maleate | Axon 2601
CAS [1312991-76-6]
MF C22H29NO2.C4H4O4MW 455.54
Purity:
99%
Optical purity:
99.5% de
Soluble in water and DMSO
Description
Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit; The HCl salt of RO 25-6981 is available as well (Axon 1314)
KEYWORDS: RO 25-6981 maleate | Supplier | NR2B antagonist | RO25-6981 |CAS[1312991-76-6] | [169274-78-6] | Glutamate | NMDA | Antagonist | Ion Channel | | axonmedchem |
| CHPG - (RS)-2-Chloro-5-hydroxyphenylglycine | α-Amino-2-chloro-5-hydroxybenzeneacetic acid | Axon 2691
CAS [170846-74-9]
MF C8H8ClNO3MW 201.61
Purity:
98%
Soluble in DMSO
Description
The mGluR5 receptor agonist CHPG selectively activates mGluR5a receptors (EC50 value of 750 μM), compared to mGluR1α receptors, when expressed in CHO cells. CHPG also potentiates NMDA-induced depolarizations in rat hippocampal slices, and is suggested to act directly on mGluR5 in dopaminergic neurons to induce the release of DA. Also CHPG promotes proliferation of human embryonic cortical NSCs with activation of the MAPKs signaling pathway.
KEYWORDS: CHPG | supplier | mGluR5 agonist | CAS [170846-74-9] | Glutamate | mGluR5 | Agonist | Receptors | CAS [1303993-73-8] | CHO | Hippocampus | | axonmedchem |
| CNQX disodium salt | Axon 2522
CAS [479347-85-8]
MF C9H2N4Na2O4MW 276.12
Purity:
99%
Soluble in water and DMSO
Description
A competitive AMPA/kainate receptor antagonist. Water soluble form of CNQX (Axon 1200)
KEYWORDS: CNQX disodium salt | supplier | AMPA/Kainate antagonist | CAS [479347-85-8] | [115066-14-3] | Glutamate | AMPA | Antagonist | Ion Channels | Axon 1200 | | axonmedchem |
| CTEP - RO 4956371 | Axon 1972
CAS [871362-31-1]
MF C19H13ClF3N3OMW 391.77
Purity:
99%
Soluble in DMSO
Description
Potent, orally bioavailable, long lasting and selective mGluR5 allosteric antagonist or negative allosteric modulator; CTEP binds mGluR5 with low nanomolar affinity and shows >1000-fold selectivity against other targets, including all known mGlu receptorsCTEP has considerably improved properties over older mGluR5 antagonists such as MPEP (Axon 1222) and Fenobam (Axon 1345)
KEYWORDS: CTEP | supplier | NAM of mGluR5 | RO 4956371 | RO4956371 | CAS [871362-31-1] | Glutamate | mGluR5 | NAM | allosteric modulator | mpep | fenobam | long lasting | | axonmedchem |
| VU 0357121 | Axon 1894
CAS [433967-28-3]
MF C17H17F2NO2MW 305.32
Purity:
99%
Soluble in DMSO
Description
Potent positive allosteric modulator (PAM) of metabotropic glutamate receptor subtype 5 (mGluR5) (EC50: 33 nM). Binds to a site distinct from that bound by MPEP (Axon 1222)
References
Certificates
Categories
Extra info
AS Hammond et al. Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chem. Neurosci. 2010, 1(10), 702-716.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR5
C3
Positive allosteric modulator (PAM) of mGluR5
Chemical name
4-butoxy-N-(2,4-difluorophenyl)benzamide
Parent CAS No.
[433967-28-3]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| TFB-TBOA | Axon 2640
CAS [480439-73-4]
MF C19H17F3N2O6MW 426.34
Purity:
100%
Optical purity:
>97% d.e.
Soluble in 0.1N NaOH(aq) and DMSO
Description
Very potent blocker for the human excitatory amino acid transporters (IC50 values 22 nM, 17 nM, and 300 nM, for EAAT1, EAAT2, and EAAT3, respectively). TFB-BOA is more potent at inhibiting EAAT1 and EAAT2 compared with L-TBOA (Axon 2427), and induced spontaneous epileptiform discharges and convulsive behaviors in mice. An important tool for elucidation of the physiological roles of EAATs and their contribution to the etiology of neuronal disorders.
KEYWORDS: TFB-TBOA | supplier | EAAT blocker | L-TFB-TBOA | CAS [480439-73-4] | Glutamate | EAAT1 | EAAT2 | Blocker | excitatory amino acid transporter | convulsion | neuronal | CNS | | axonmedchem |
| VU 0364770 | Axon 1845
CAS [61350-00-3]
MF C12H9ClN2OMW 232.67
Purity:
99%
Soluble in DMSO
Description
A systemically active positive allosteric modulator (PAM) of metabotropic glutamate receptor subtype 4 (mGluR4) (EC50: 290 nM); showed efficacy alone or when administered in combination with L-DOPA or an adenosine 2A (A2A) receptor antagonist, in several rodent PD models
References
Certificates
Categories
Extra info
CK Jones et al. The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical (...). J. Pharmacol. Exp. Ther. 2012, 340(2), 404-21.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR4
C3
Positive allosteric modulator (PAM) of mGluR4
Chemical name
N-(4-chlorophenyl)picolinamide
Parent CAS No.
[61350-00-3]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| VU 0361737 | Axon 1842
CAS [1161205-04-4]
MF C13H11ClN2O2MW 262.69
Purity:
99%
Soluble in DMSO
Description
Centrally penetrant and selective positive allosteric modulator (PAM) of metabotropic glutamate receptor subtype 4 (mGluR4); displayed submicromolar potency at both human and rat mGluR4
References
Certificates
Categories
Extra info
DW Engers et al. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J. Med. Chem. 2009, 52(14), 4115-4118.
DW Engers et al. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-Acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (...). J. Med. Chem. 2011, 54(4), 1106-1110.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR4
C3
Positive allosteric modulator (PAM) of mGluR4
Chemical name
N-(4-chloro-3-methoxyphenyl)picolinamide
Parent CAS No.
[1161205-04-4]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| VU 0364439 | Axon 1830
CAS [1246086-78-1]
MF C18H13Cl2N3O3SMW 422.29
Purity:
99%
Soluble in DMSO
Description
Very potent positive allosteric modulator (PAM) of metabotropic glutamate receptor subtype 4 (mGluR4) (EC50: 19.8 nM)
References
Certificates
Categories
Extra info
DW Engers et al. Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorg. Med. Chem. Lett. 2010, 20(17), 5175-5178.
AJ Robichaud et al. Recent Progress on the Identification of Metabotropic Glutamate 4 Receptor Ligands and Their Potential Utility as CNS Therapeutics. ACS Chem. Neurosci. 2011, 2(8), 433–449.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR4
C3
Positive allosteric modulator (PAM) of mGluR4
Chemical name
N-(3-chloro-4-(N-(2-chlorophenyl)sulfamoyl)phenyl)picolinamide
Parent CAS No.
[1246086-78-1]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| VU 0360223 | Axon 1795
CAS [1274859-33-4]
MF C15H9FN2SMW 268.31
Purity:
99%
Soluble in DMSO
Description
Potent and selective metabotropic glutamate receptor subtype 5 (mGluR5) antagonist or negative allosteric modulator (NAM) (IC50: 61 nM)
References
Certificates
Categories
Extra info
CW Lindsley et al. (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu5: discovery of a new tool compound with activity in the OSS mouse model of addiction. ACS Chem. Neurosci. 2011, 2(8), 471-482.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR5
C3
mGluR5 antagonist
Chemical name
3-fluoro-5-(2-methylbenzo[d]thiazol-5-yl)benzonitrile
Parent CAS No.
[1274859-33-4]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| AZ 12216052 | Axon 1747
CAS [1290628-31-7]
MF C19H22BrNOSMW 392.35
Purity:
98%
Soluble in DMSO
Description
A positive allosteric modulator (PAM) of metabotropic glutamate receptor subtype 8 (mGluR8)
References
Certificates
Categories
Extra info
RM Duvoisin et al. Opposing roles of mGluR8 in measures of anxiety involving non-social and social challenges. Behav. Brain Res. 2011, 221(1), 50-54.
RM Duvoisin et al, Acute pharmacological modulation of mGluR8 reduces measures of anxiety. Behav. Brain Res. 2010, 212(2), 168-173.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR8
C3
Positive allosteric modulator (PAM) of mGluR8
Chemical name
2-(4-bromobenzylthio)-N-(4-sec-butylphenyl)acetamide
Parent CAS No.
[1290628-31-7]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| S 18986 | Axon 1788
CAS [175340-20-2]
MF C10H12N2O2SMW 224.28
Purity:
99%
Optical purity:
>99% ee
Soluble in DMSO
Description
Positive allosteric modulator of AMPA receptor with cognitive-enhancing effects; neuroprotective; long-acting and with good oral availability
References
Certificates
Categories
Extra info
B Lockhart et al. (S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide: (S18986-1) a positive modulator of AMPA receptors enhances (S)-AMPA-mediated [3H]noradrenaline release (...). Eur. J. Pharmacol. 2000, 401(2), 145–153.
C Lebrun et al. Effects of S 18986-1, a novel cognitive enhancer, on memory performances in an object recognition task in rats. Eur. J. Pharmacol. 2000, 401(2), 205–212.
SM Gupta et al. GAP-43 is essential for the neurotrophic effects of BDNF and positive AMPA receptor modulator S18986. Cell Death Differ. 2009, 16(4), 624–637.
KD Destot-Wong et al. The AMPA receptor positive allosteric modulator, S18986, is neuroprotective against neonatal excitotoxic and inflammatory brain damage through BDNF synthesis. Neuropharmacology 2009, 57(3), 277–286.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
AMPA
Unclassified
Positive allosteric modulator of AMPA receptor
Chemical name
(+)-(S)-2,3,3a,4-Tetrahydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazine-5,5-dioxide
Parent CAS No.
[175340-20-2]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| DHPG, (RS)-3,5- | Axon 1739
CAS [146255-66-5]
MF C8H9NO4MW 183.16
Purity:
99%
Soluble in water and DMSO
Description
Selective group I metabotropic glutamate receptor agonist which activates both mGluR1 and mGluR5. More specifically, the agonist activity is found only in its S-enantiomer, (S)-3,5-DHPG (Axon 1740) .
References
Certificates
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Extra info
I Ito et al. 3,5-Dihydroxyphenyl-glycine: a potent agonist of metabotropic glutamate receptors. Neuroreport. 1992, 3(11), 1013-1016.
DD Schoepp et al. 3,5-dihydroxyphenylglycine is a highly selective agonist for phosphoinositide-linked metabotropic glutamate receptors in the rat hippocampus. J. Neurochem. 1994, 63(2), 769-772.
C Wiśniewski and H Car. (S)-3,5-DHPG: a review. CNS Drug Rev. 2002, 8(1), 101–116.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR5
mGluR1
C3
mGluR1 and mGluR5 agonist (rac. Axon 1740)
Chemical name
2-amino-2-(3,5-dihydroxyphenyl)acetic acid
Parent CAS No.
[146255-66-5]
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10 mg
€80.00
In Stock | | axonmedchem |
| VU 29 | Axon 1425
CAS [890764-36-0]
MF C22H16N4O3MW 384.39
Purity:
99%
Soluble in DMSO
Description
A Positive Allosteric Modulator (PAM) of metabotropic glutamate receptor subtype 5 (mGluR5)
References
Certificates
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Extra info
JE Ayala et al. A Positive Allosteric Modulator of mGluR5 Potentiates DHPG-induced Long Term Depression at the Schaffer Collateral–CA1 Synapse of the Rat Hippocampus. FASEB J. 2008, 22, 714.4.
Y Chen et al. Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol. Pharmacol. 2007, 71, 1389–1398.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR5
C3
Positive allosteric modulator (PAM) of mGluR5
Chemical name
N-(1,3-diphenyl-1H-pyrazol-5-yl)-4-nitro-benzamide
Parent CAS No.
[890764-36-0]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| CPPHA | Axon 1431
CAS [693288-97-0]
MF C22H15ClN2O4MW 406.82
Purity:
99%
Soluble in DMSO
Description
A positive allosteric modulator (PAM) of metabotropic glutamate receptor subtype 5 (mGluR5)
References
Certificates
Categories
Extra info
J O'Brien et al. A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J. Pharmacol. Exp. Ther. 2004, 309, 568-577.
Y Chen et al. N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) Acts through a Novel Site as a Positive Allosteric Modulator of Group 1 Metabotropic Glutamate Receptors. Mol. Pharmacol. 2008, 73, 909-918.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR5
C3
Positive allosteric modulator (PAM) of mGluR5
Chemical name
N-[4-Chloro-2-(1,3-dioxo-1,3-dihydro-isoindol-2-ylmethyl)-phenyl]-2-hydroxy-benzamide
Parent CAS No.
[693288-97-0]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| GYKI 53655 - LY 300168 | Axon 1374
CAS [143692-18-6]
MF C19H20N4O3MW 352.39
Purity:
99%
Soluble in DMSO and Ethanol
Description
Selective AMPA receptor antagonist; a more useful tool than NBQX for the study of AMPA receptor-mediated processes in vivo
References
Certificates
Categories
Extra info
BA Chizh et al. A comparison of intravenous NBQX and GYKI 53655 as AMPA antagonists in the rat spinal cord. Br. J. Pharmacol. 1994, 112(3), 843-6.
AD Kovács and G Szabó. GYKI 53655, a 2,3-benzodiazepine, non-competitively protects cultured neurones against AMPA toxicity. Eur. J. Pharmacol. 1997, 331(1), 93-96.
Szabados et al. Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405 and GYKI 53655. Brain. Res. Bull. 2001, 55 387.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
AMPA
Unclassified
AMPA antagonist
Chemical name
5-(4-Amino-phenyl)-8-methyl-8,9-dihydro-1,3-dioxa-6,7-diaza-cyclohepta[f]indene-7-carboxylic acid methylamide
Parent CAS No.
[143692-18-6]
Order
Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| Lamotrigine | Axon 1353
CAS [84057-84-1]
MF C9H7Cl2N5MW 256.09
Purity:
99%
Soluble in DMSO
Description
Glutamate antagonist and sodium channel blocker; an anticonvulsant drug
References
Certificates
Categories
Extra info
L Barbosa et al. A double-blind, randomized, placebo-controlled trial of augmentation with lamotrigine or placebo in patients concomitantly treated with fluoxetine for resistant major depressive episodes. J. Clin. Psychiatry. 2003, 6(4), 403–407.
WJ Curry and DL Kulling. Newer Antiepileptic Drugs: Gabapentin, Lamotrigine, Felbamate, Topiramate and Fosphenytoin. Am. Fam. Physician. 1998, 57(3), 513.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
NMDA
Unclassified
Glutamate antagonist; Na+ channel blocker
Chemical name
6-(2,3-Dichloro-phenyl)-[1,2,4]tria
zine-3,5-diamine
Parent CAS No.
[84057-84-1]
Order
Size
Unit Price
Stock
10 mg
€60.00
In Stock | | axonmedchem |
| Fenobam - MCN 3377-98 | NPL 2009 | Axon 1345
CAS [57653-26-6]
MF C11H11ClN4O2MW 266.68
Purity:
99%
Soluble in DMSO
Description
Potent and selective antagonist for metabotropic glutamate receptor subtype 5 (mGluR5).
KEYWORDS: Fenobam | supplier | mGluR5 antagonist | MCN 3377-98 | NPL 2009 | MCN3377-98 | NPL2009 | MCN-3377-98 | NPL-2009 | CAS [57653-26-6] | Glutamate | mGlu5 antagonist | mGluR5 | mGlu5 | Antagonist | Receptors | | axonmedchem |
| YM 90K hydrochloride | Axon 1312
CAS [154164-30-4]
MF C11H7N5O4.HClMW 309.67
Purity:
98%
Moderately soluble in DMSO
Description
AMPA antagonist with neuro-protective effect
References
Certificates
Categories
Extra info
Yoa, H. et al. AMPA receptor antagonist, YM90K, reduces infarct volume in thrombotic distal middle cerebral artery occlusion in spontaneously hypertensive rats. Brain Res. 1997, 753(1), 80-85.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
AMPA
Unclassified
AMPA antagonist
Chemical name
6-Imidazol-1-yl-7-nitro-1,4-dihydro-quinoxaline-2,3-dione hydrochloride
Parent CAS No.
[143151-35-3]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| RO 25-6981 hydrochloride | Axon 1314
CAS [919289-58-0]
MF C22H29NO2.HClMW 375.93
Purity:
99%
Optical purity:
99.5% de
Soluble in water and DMSO
Description
Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit; Optimal salt form, which is more water soluble than its maleate salt form (Axon 2601)
KEYWORDS: RO 25-6981 hydrochloride | Supplier | NR2B antagonist | RO25-6981 HCl | CAS [1312991-76-6] | [169274-78-6] | Glutamate | NMDA | Antagonist | Ion Channel | | axonmedchem |
| YM 298198 hydrochloride | Axon 1260
CAS [299901-50-1]
MF C18H22N4OS.HClMW 378.92
Purity:
99%
Soluble in water and DMSO
Description
Selective mGlu1 antagonist
References
Certificates
Categories
Extra info
Fukunaga et al. Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices. Br. J. Pharmacol. 2007, 151(6), 870-876.
Kohara et al. Radioligand binding properties and pharmacological characterization of 6-Amino-N-cyclohexyl-N,3-dimethyl-thiazolo[3,2-a]-benzimidazole-2-carboxamide (YM-298198). J. Pharmacol. Exp. Ther. 2005, 315, 163.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR1
C3
mGluR1 antagonist
Chemical name
6-Amino-3-methyl-benzo[4,5]imidazo[2,1-b]thiazole-2-carboxylic acid cyclohexyl-methyl-amide hydrochloride
Parent CAS No.
[748758-45-4]
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Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| YM 298198 hydrochloride, desmethyl | Axon 1259
CAS [1177767-57-5]
MF C17H20N4OS.HClMW 364.89
Purity:
98%
Soluble in water
Description
Derivative of YM-298198 (Axon 1260), a selective and noncompetitive mGluR1 antagonist
KEYWORDS: Desmethyl YM 298198 hydrochloride | 299901-57-8 | 1177767-57-5 | Axon 1259 | mGluR1 antagonist | Supplier | Axon1259 | YM298198 | desmethyl | mGluR1 | | axonmedchem |
| N 20C hydrochloride | Axon 1249
CAS [1177583-87-7]
MF C17H20N2O.HClMW 304.81
Purity:
98%
No solubility data
Description
Non-competitive NMDA glutamate receptor antagonist
References
Certificates
Categories
Extra info
R Planells-Cases et al. A novel N-methyl-D-aspartate receptor open channel blocker with in vivo neuroprotectant activity. J. Pharmacol. Exp. Ther. 2002, 302, 163.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
NMDA
Unclassified
NMDA antagonist
Chemical name
2-(3,3-Diphenyl-propylamino)-acetamide hydrochloride
Parent CAS No.
[76991-05-4]
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Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Gavestinel - GV 150526A | Axon 1262
CAS [153436-38-5]
MF C18H11Cl2N2NaO3MW 397.19
Purity:
99%
Soluble in DMSO
Description
In vivo potent and selective antagonist of glycine site of NMDA receptor; orally bioavailable; neuroprotective in animal models of ischaemic stroke
References
Certificates
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Extra info
Mugnaini et al. Receptor binding characteristics of the novel NMDA receptor glycine site antagonist [3H]GV150526A in rat cerebral cortical membranes. Eur. J. Pharmacol. 2002, 391, 233.
Kajbaf et al. Pharmacokinetics, metabolism and excretion of the glycine antagonist GV150526A in rat and dog. Xenobiotica. 2003, 33, 415.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
NMDA
Unclassified
NMDA antagonist (glycine site)
Chemical name
4,6-Dichloro-3-((E)-2-phenylcarbamoyl-vinyl)-1H-indole-2-carboxylic acid sodium salt
Parent CAS No.
[153436-22-7]
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Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| Eliprodil - SL 820715 | Axon 1246
CAS [119431-25-3]
MF C20H23ClFNOMW 347.85
Purity:
99%
Soluble in DMSO
Description
Non-competitive NMDA antagonist, selective for NR2B type; Neuroprotective agent.
KEYWORDS: Eliprodil | supplier | NMDA antagonist | SL 820715 | SL820715 | SL-820715 | CAS [119431-25-3] | Glutamate | Ion Channels | Non-competitive | NR2B | Neuroprotective | | axonmedchem |
| LY 367385, (±)- | Axon 1224
CAS [198419-90-8]
MF C10H11NO4MW 209.20
Purity:
98%
Soluble in water
Description
LY367385 [198419-91-9] is a selective mGlu1a antagonist
References
Certificates
Categories
Extra info
V. Bruno et al. Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4-carboxy phenylglycine (LY367385). Neuropharmacology 1999, 38, 199.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR1A
C3
mGluR1a antagonist
Chemical name
4-(Amino-carboxy-methyl)-3-methyl-benzoic acid
Parent CAS No.
[198419-90-8]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| CFM 2 | Axon 1217
CAS [178616-26-7]
MF C17H17N3O3MW 311.34
Purity:
98%
Soluble in DMSO
Description
Potent and selective AMPA antagonist
References
Certificates
Categories
Extra info
De Sarro et al. Anticonvulsant activity and plasma level of 2,3-benzodiazepin-4-ones (CFMs) in genetically epilepsy-prone rats. Pharmacol. Biochem. Behav. 1999, 63, 621.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
AMPA
Unclassified
AMPA antagonist
Chemical name
1-(4-Amino-phenyl)-7,8-dimethoxy-3,5-dihydro-benzo[d][1,2]diazepin-4-one
Parent CAS No.
[178616-26-7]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| MPEP hydrochloride | Axon 1222
CAS [219911-35-0]
MF C14H11N.HClMW 229.70
Purity:
99%
Soluble in water, DMSO, and Ethanol
Description
Potent and selective antagonist for metabotropic glutamate receptor subtype 5 (mGluR5); Systemically active in vivo
References
Certificates
Categories
Extra info
P. Bäckström et al. mGluR5 Antagonist MPEP Reduces Ethanol-Seeking and Relapse Behavior. Neuropsychopharmacology 2004, 29, 921–928.
PM Lea et al. Neuroprotective activity of the mGluR5 antagonists MPEP and MTEP against acute excitotoxicity differs and does not reflect actions at mGluR5 receptors. Br. J. Pharmacol. 2005, 145, 527-534.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR5
C3
mGluR5 antagonist
Chemical name
2-Methyl-6-phenylethynyl-pyridine hydrochloride
Parent CAS No.
[96206-92-7]
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Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| DNQX | Axon 1201
CAS [2379-57-9]
MF C8H4N4O6MW 252.14
Purity:
99%
Soluble in DMSO
Description
AMPA/Kainate antagonist
References
Certificates
Categories
Extra info
Honore et al. Quinoxalinediones: Potent competitive non-NMDA glutamate receptor antagonists. Science 1988, 241, 701.
Long et al. Effect of 6-cyano-2,3-dihydroxy-7-nitro-quinoxaline (CNQX) on dorsal root-, NMDA-, kainate- and quisqualate-mediated depolarization of rat motoneurones in vitro. Br. J. Pharmacol. 1990, 100, 850-854.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
AMPA
Unclassified
AMPA/Kainate antagonist
Chemical name
6,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione
Parent CAS No.
[2379-57-9]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| CNQX | Axon 1200
CAS [115066-14-3]
MF C9H4N4O4MW 232.15
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Competitive AMPA/kainate receptor antagonist.
The water soluble disodium salt of CNQX (Axon 2522) is available as well
KEYWORDS: CNQX | supplier | AMPA/Kainate antagonist | CAS [115066-14-3] - [479347-85-8] | Glutamate | AMPA | Antagonist | Ion Channels | Kainate | | axonmedchem |
| MHY 908 | Axon 2402
CAS [1393371-39-5]
MF C17H14ClNO3SMW 347.82
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Dual PPARα/γ agonist, and potent inhibitor of melanogenesis by inhibition of mushroom tyrosinase activity (IC50 value 8.19 μM). MHY908 more potently activated PPARα and PPARγ than fenofibrate and rosiglitazone, respectively, and enhanced the binding and transcriptional activity of PPARα and -γ in AC2F cells. It reduced serum glucose, triglyceride, and insulin levels, however increased adiponectin levels without body weight gain. In addition, MHY 908 significantly improved hepatic steatosis by enhancing CPT-1 levels. Remarkably, MHY-908 reduced endoplasmic reticulum (ER) stress and c-Jun N-terminal kinase (JNK) activation, and subsequently reduced insulin resistance.
References
Certificates
Categories
Extra info
M.H. Park et al. Potent anti-diabetic effects of MHY908, a newly synthesized PPAR α/γ dual agonist in db/db mice. PLoS One. 2013 Nov 14;8(11):e78815.
M.H. Park et al. Inhibition of melanogenesis by 2-[4-(5-chlorobenzo[d]thiazol-2-yl)phenoxy]-2-methylpropanoic acid (MHY908). Arch Pharm Res. 2014 Dec 14. [Epub ahead of print]
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
PPAR
Tyrosinase
NR1C; EC 1.14.18.1
Dual PPARα/γ agonist, and potent inhibitor of mushroom tyrosinase
Chemical name
2-(4-(5-chlorobenzo[d]thiazol-2-yl)phenoxy)-2-methylpropanoic acid
Parent CAS No.
[1393371-39-5]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Ifenprodil L-(+)-tartrate | Axon 1156
CAS [23210-58-4]
MF C21H27NO2.½C4H6O6MW 400.49
Purity:
99%
Soluble in water and DMSO
Description
NMDA antagonist; selectively blocks NMDA receptors containing the NR2B subunit; neuroprotective agent
References
Certificates
Categories
Extra info
Kurihara et al. Selective dysfunction of the vagal component of the baroreflex following cerebral ischemia: protection by ifenprodil and flunarizine. Eur. J. Pharmacol. 1990, 190, 23.
Carter et al. Ifenprodil and SL 82.0715 are antagonists at the polyamine site of the N-methyl-D-aspartate (NMDA) receptor. Eur. J. Pharmacol. 1989, 164, 611.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
NMDA
Unclassified
NMDA antagonist
Chemical name
4-((1R*,2S*)-2-(4-benzylpiperidin-1-yl)-1-hydroxypropyl)phenol hemi-L-(+)-tartrate
Parent CAS No.
[23210-56-2]
Order
Size
Unit Price
Stock
10 mg
€55.00
In Stock | | axonmedchem |
| ZLN 005 | Axon 2379
CAS [49671-76-3]
MF C17H18N2MW 250.34
Purity:
99%
Soluble in DMSO
Description
Selective transcriptional regulator of peroxisome proliferator–activated receptor-γ coactivator-1α (PGC-1α). ZLN005 selectively stimulated the expression of PGC-1α and downstream genes in skeletal muscle cells, and led to changes in glucose uptake, and fatty acid oxidation in L6 myotubes in a AMPK dependent manner. Since ZLN 005 did not increase the expression of the PGC-1α gene in rat primary hepatocytes, it is hypothesized that expression of PGC-1α was regulated in a cell type–specific manner. ZLN005 exerts promising therapeutic effects for treating type 2 diabetes, as PGC-1α is a powerful transcriptional coregulator of GLUT4 and mitochondrial genes, a crucial player in the field of glucose uptake in skeletal muscle.
References
Certificates
Categories
Extra info
L.N. Zhang et al. Novel small-molecule PGC-1α transcriptional regulator with beneficial effects on diabetic db/db mice. Diabetes. 2013, 62, 1297-1307.
L.N. Zhang et al. Novel small-molecule AMP-activated protein kinase allosteric activator with beneficial effects in db/db mice. PLoS One. 2013, 8, e72092.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Transcription Factors
PGC
PPARGC1A
Selective transcriptional regulator of peroxisome PPAR-γ coactivator-1α (PGC-1α).
Chemical name
2-(4-tert-butylphenyl)-1H-benzo[d]imidazole
Parent CAS No.
[49671-76-3]
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Size
Unit Price
Stock
10 mg
€45.00
In Stock | | axonmedchem |
| GW 9662 | Axon 2262
CAS [22978-25-2]
MF C13H9ClN2O3MW 276.68
Purity:
100%
Soluble in DMSO and Ethanol
Description
Potent PPARγ antagonist (IC50 values 3.3 nM, 32 nM and 2000 nM for PPARγ, PPARα, and PPARδ, respectively) which inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARγ agonist rosiglitazone, independently of PPARγ activation. GW 9662 profoundly improved healing and induced angiogenesis in human mesenchymal stem cells (hMSCs), and reversed the protection of endotoxin (lipopolysaccharide, LPS) in a model of renal ischemia-reperfusion.
References
Certificates
Categories
Extra info
U. Krause et al. Pharmaceutical modulation of canonical Wnt signaling in multipotent stromal cells for improved osteoinductive therapy. PNAS USA 2010, 107, 4147-4152.
J.M. Seargent et al. GW9662, a potent antagonist of PPARγ, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARγ agonist rosiglitazone, independently of PPARγ activation. Br. J. Pharmacol. 2004, 143, 933-937.
M. Collino et al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005, 68, 529-536.
L.M. Leesnitzer et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochem. 2002, 41, 6640-6650.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
PPAR
NR1C
Selective PPARγ antagonist
Chemical name
2-chloro-5-nitro-N-phenylbenzamide
Parent CAS No.
[22978-25-2]
Order
Size
Unit Price
Stock
10 mg
€60.00
In Stock | | axonmedchem |
| LDN 212320 | Axon 2260
CAS [894002-50-7]
MF C17H15N3SMW 293.39
Purity:
100%
Soluble in DMSO
Description
LDN 212320 is an activator of excitatory amino acid transporter 2 (EAAT2) translation and has significant neuroprotective effects in vivo.
References
Certificates
Categories
Extra info
X. Xing et al. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators. Bioorg. Med. Chem. Lett. 2011, 21, 5774-5777.
C.L. Lin et al. Glutamate transporter EAAT2: a new target for the treatment of neurodegenerative diseases. Future Med. Chem. 2012, 4, 1689-1700.
Certificate of Analysis
Material Safety Data Sheet
CNS
Unclassified
EAAT
Activator of EAAT2 translation; neuroprotectant
Chemical name
3-(2-methylbenzylthio)-6-(pyridin-2-yl)pyridazine
Parent CAS No.
[894002-50-7]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |