A potent

AMG 837 – 25 mg

Brand:
Cayman
CAS:
865231-46-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

AMG 837 is a potent, orally bioavailable partial agonist at GPR40 (FFAR1; EC50 = 13 nM) that is highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM) in a calcium flux assay using CHO cells transfected with the human receptor.{34388,34389} GPR40 is a G protein-coupled free fatty acid receptor localized mainly on pancreatic islet cells that activates the Gq signaling pathway. In rats, AMG 837 increases insulin release when glucose levels are elevated, but it failed to do so in healthy volunteers during Phase I clinical trials.{34389,34390}  

 

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Description

A potent, orally bioavailable GPR40 agonist (EC50 = 13 nM); activates the Gq pathway; highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM); increases insulin release in rats when glucose is elevated

Formal name: βS-1-propyn-1-yl-4-[[4′-(trifluoromethyl)[1,1′-biphenyl]-3-yl]methoxy]-benzenepropanoic acid

Synonyms: 

Molecular weight: 438.4

CAS: 865231-46-5

Purity: ≥98%

Formulation: A crystalline solid

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

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