| Identification | Back Directory | [Name]
Cyclopropa[4,5]cyclopenta[1,2-c]pyridine-6-carboxylic acid, 3-[[2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-5,5a,6,6a-tetrahydro-, (5aS,6R,6aR)- | [CAS]
1544739-76-5 | [Synonyms]
Cyclopropa[4,5]cyclopenta[1,2-c]pyridine-6-carboxylic acid, 3-[[2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-5,5a,6,6a-tetrahydro-, (5aS,6R,6aR)- | [Molecular Formula]
C29H31NO6S | [MOL File]
1544739-76-5.mol | [Molecular Weight]
521.62 |
| Hazard Information | Back Directory | [Description]
MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects. | [Uses]
(5aS,6R,6aR)-MK-8666 is a selective GPR40 agonist with activity in promoting fatty acid-induced insulin secretion in pancreatic β cells and intestinal enteroendocrine cells. (5aS,6R,6aR)-MK-8666 has been studied for the inhibition of type 2 diabetes and has shown significant blood glucose lowering effects. Although (5aS,6R,6aR)-MK-8666 is considered to have potential inhibitory advantages, its development was stopped in Phase I clinical trials due to liver safety issues[1]. | [References]
[1] Bioactivation of GPR40 Agonist MK-8666: Formation of Protein Adducts in Vitro from Reactive Acyl Glucuronide and Acyl CoA Thioester |
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