Molecular structure of GW 9508, CAS Number: 885101-89-3
GW 9508 (CAS 885101-89-3)
Alternate Names:
3-(4-(((3-(Phenoxy)phenyl)methyl)amino)phenyl)propanoic acid; GPR40 Agonist
Application:
GW 9508 is an aminophenylpropanoate agonist at the GRP40/FFA1 receptor
CAS Number:
885101-89-3
Purity:
≥98%
Molecular Weight:
347.4
Molecular Formula:
C22H21NO3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40 (EC50 50 nM) with much reduced activity towards family members GRP120 (EC50 3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other fatty acid and prostaglandin receptors. Shown to induces GPR40-dependent Ca2+ mobilization in HEK-293 cells and potentiate glucose-stimulated insulin secretion in MIN6 cells.
GW 9508 (CAS 885101-89-3) References
- Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. | Briscoe, CP., et al. 2006. Br J Pharmacol. 148: 619-28. PMID: 16702987
- Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor. | McKeown, SC., et al. 2007. Bioorg Med Chem Lett. 17: 1584-9. PMID: 17240142
- Identification of residues important for agonist recognition and activation in GPR40. | Sum, CS., et al. 2007. J Biol Chem. 282: 29248-55. PMID: 17699519
- Insight into analysis of interactions of GW9508 to wild-type and H86F and H137F GPR40: a combined QM/MM study and pharmacophore modeling. | Lu, SY., et al. 2011. J Mol Graph Model. 29: 818-25. PMID: 21334233
- A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. | Fujita, T., et al. 2011. J Invest Dermatol. 131: 1660-7. PMID: 21593768
- Multiple mechanisms of GW-9508, a selective G protein-coupled receptor 40 agonist, in the regulation of glucose homeostasis and insulin sensitivity. | Ou, HY., et al. 2013. Am J Physiol Endocrinol Metab. 304: E668-76. PMID: 23341496
- GW9508, a free fatty acid receptor agonist, specifically induces cell death in bone resorbing precursor cells through increased oxidative stress from mitochondrial origin. | Philippe, C., et al. 2013. Exp Cell Res. 319: 3035-41. PMID: 23973666
- The fish oil ingredient, docosahexaenoic acid, activates cytosolic phospholipase A₂ via GPR120 receptor to produce prostaglandin E₂ and plays an anti-inflammatory role in macrophages. | Liu, Y., et al. 2014. Immunology. 143: 81-95. PMID: 24673159
- Anti-atherosclerotic action of GW9508 - Free fatty acid receptors activator - In apoE-knockout mice. | Suski, M., et al. 2019. Pharmacol Rep. 71: 551-555. PMID: 31129318
- G-protein-coupled receptor 40 agonist GW9508 potentiates glucose-stimulated insulin secretion through activation of protein kinase Cα and ε in INS-1 cells. | Hashimoto, T., et al. 2019. PLoS One. 14: e0222179. PMID: 31498851
- GW9508 ameliorates cognitive impairment via the cAMP-CREB and JNK pathways in APPswe/PS1dE9 mouse model of Alzheimer's disease. | Gong, Y., et al. 2020. Neuropharmacology. 164: 107899. PMID: 31809762
- The GPR40 Agonist GW9508 Enhances Neutrophil Function to Aid Bacterial Clearance During E. coli Infections. | Souza, PR., et al. 2020. Front Immunol. 11: 573019. PMID: 33133087
- FFAR1 activation attenuates histamine-induced myosin light chain phosphorylation and cortical tension development in human airway smooth muscle cells. | Xu, S., et al. 2020. Respir Res. 21: 317. PMID: 33256729
- GPR120 Agonist GW9508 Ameliorated Cellular Senescence Induced by ox-LDL. | Liu, R., et al. 2020. ACS Omega. 5: 32195-32202. PMID: 33376857
- GW9508 ameliorates cognitive dysfunction via the external treatment of encephalopathy in Aβ1-42 induced mouse model of Alzheimer's disease. | Gong, Y., et al. 2021. Eur J Pharmacol. 909: 174362. PMID: 34297968
Inhibitor of:
MrgA1.Activator of:
CALCA, GPR120, GPR40, and NPC1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GW 9508, 10 mg | sc-203069 | 10 mg | $128.00 |