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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

GW-1100

HY-50691

(GW1100; GW1100)

GW-1100
GW-1100 Chemical Structure

GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.

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GW-1100 Data Sheet

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Purity: 98.13%

GW-1100

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Biological Activity of GW-1100

GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.
IC50 value:
Target: GPR40
GPR40 is a G protein-coupled receptor (GPCR) that is activated by saturated and unsaturated long chain fatty acids. It is thought to play a role in the potentiation of insulin secretion by fatty acids in a glucose-sensitive manner. GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99. However at concentrations up to 10 μM, GW 1100 has no effect on GPR120-mediated stimulation of intracellular Ca2+ release induced by either GW 9508 or linoleic acid. In the MIN6 mouse insulinoma cell line, 1 μM GW 1100 inhibits the potentiating effects of GW 9508 and linoleic acid on glucose-stimulated insulin secretion.

[1]. Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist.Molecular Pharmacology (2007), 71(4), 994

[2]. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. British Journal of Pharmacology (2006), 148(5), 619-628.

[3]. Zhao Y, Song Y, Shen X, Liao J.Feasible Synthesis of Antagonist of GPR40 by Constructing 2-Thiouracil Ring viaAcid Mediated Cyclization.Heterocycles. 2011 May 1;83(5):1145-1151.

[4]. Briscoe CP, Peat AJ, McKeown SC, Corbett DF, Goetz AS, Littleton TR, McCoy DC, Kenakin TP, Andrews JL, Ammala C, Fornwald JA, Ignar DM, Jenkinson S.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. Epub 2006 May 15.

Products are for research use only. Not for human use. We do not sell to patients.

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