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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.
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.
|M.Wt||520.58||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||1.9209 mL||9.6047 mL||19.2093 mL|
|5 mM||0.3842 mL||1.9209 mL||3.8419 mL|
|10 mM||0.1921 mL||0.9605 mL||1.9209 mL|
. 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
. 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.
. 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.
GPR40 Activator 1 is a potent GPR40 activator for treatment of type 2 diabetes.
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
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.
TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 (mu)M.
TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
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