A selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells (pIC50 = 5.99) without effecting those mediated by GPR120 at concentrations up to 10 μM; at 1 μM

GW 1100 – 10 mg

Brand:
Cayman
CAS:
306974-70-9
Storage:
-20
UN-No:
Non-Hazardous - /

GPR40 (free fatty acid receptor 1; FFAR1) 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 (FFAR4), 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.{14194} 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.{14194}  

 

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SKU: 10008908 - 10 mg Category:

Description

A selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells (pIC50 = 5.99) without effecting those mediated by GPR120 at concentrations up to 10 μM; at 1 μM, inhibits the potentiating effects of GPR agonist, GW 9508 and linoleic acid on glucose-stimulated insulin secretion

Formal name: 4-[5-[(2-ethoxy-5-pyrimidinyl)methyl]-2-[[(4-fluorophenyl)methyl]thio]-4-oxo-1(4H)-pyrimidinyl]-benzoic acid, ethyl ester

Synonyms: 

Molecular weight: 520.6

CAS: 306974-70-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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