GW9508 Inhibitor CAS No. 885101-89-3

Cat. No.	Name	Size	Price	Add Cart
KI3675	GW9508	10 mg	$250
KI3675	GW9508	50 mg	$800

Chemical Characteristic

Product Name	GW9508
CAS No.	885101-89-3
Molecular Weight	347.41
Formula	C₂₂H₂₁NO₃
Chemical Name	4-[[(3-Phenoxyphenyl)methyl]amino]benzenepropanoic acid
Smiles	c1(ccc(cc1)NCc1cc(ccc1)Oc1ccccc1)CCC(=O)O
Chemical Structure

Biological activities

GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner ^[1]. GW9508 produces a concentration-dependent increase in intracellular Ca2+ concentrations via GPR40 receptor activation and the GPR120 receptor ^[2]. GW9508 is active as an agonist at both GPR40 and GPR120, it is approximately 100-fold selective for GPR40 with respect to GPR120. GW9508 produces a concentration-dependent increase (pEC50=6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM) ^[3]. In vivo, GW9508 can be used by 50 mg/kg in mice. In vitro, it can be used by 10 ?M in HepG2 cells ^[4].

References

[1] Zhao YF, Pei J, Chen C. 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. [2] Briscoe CP, Peat AJ, McKeown SC, 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, 148(5):619-628. [3] Fujita T, Matsuoka T, Honda 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] Ou HY, Wu HT, Hung HC, et al. Multiple mechanisms of GW-9508, a selective G protein-coupled receptor 40 agonist, in the regulation of glucose homeostasis and insulin sensitivity. Am J Physiol Endocrinol Metab. 2013, 304(6):668-676.

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