GW9508

GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities[1][2][3][4].

Product Specifications

CAS Number

[885101-89-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H318, H335, H410

Target

Free Fatty Acid Receptor; Potassium Channel

Type

Reference compound

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/GW9508.html

Purity

99.23

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(O)CCC1=CC=C(NCC2=CC=CC(OC3=CC=CC=C3)=C2)C=C1

Molecular Formula

C22H21NO3

Molecular Weight

347.41

Precautions

H302, H315, H318, H335, H410

References & Citations

[1]Briscoe CP, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148 (5) :619-28.|[2]Zhao YF, et al. Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway. J Endocrinol, 2008, 198 (3), 533-540.|[3]Fujita T, et al. A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. J Invest Dermatol, 2011, 131 (8), 1660-1667.|[4]Suski M, et al. Anti-atherosclerotic action of GW9508 - Free fatty acid receptors activator - In apoE-knockout mice. Pharmacol Rep. 2019 Aug;71 (4) :551-555.