TUG-469 is a potent free fatty acid 1 receptor agonist. TUG-469 showed a 1.7- to 3.0-times higher potency in vitro at 1321N1 cells recombinantly expressing FFA1. Both compounds increased insulin secretion from rat insulinoma INS-1 cells. TUG-469 is > 200-fold selective for FFA1 over FFA4. Finally, a single dose of 5 mg/kg TUG-469 significantly improved glucose tolerance in pre-diabetic NZO mice. TUG-469 turned out as a promising candidate for further drug development of FFA1 agonists for treatment of type 2 diabetes mellitus. Activation of the G protein-coupled free fatty acid receptor 1 (FFA1; formerly known as GPR40) leads to an enhancement of glucose-stimulated insulin secretion from pancreatic β-cells. References: Panse M, Gerst F, Kaiser G, Teutsch CA, Dolker R, Wagner R, Haring HU, Ullrich S. Activation of extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) by free fatty acid receptor 1 (FFAR1/GPR40) protects from palmitate-induced beta cell death, but plays no role in insulin secretion. Cell Physiol Biochem. 2015;35(4):1537-45. doi: 10.1159/000373969. Epub 2015 Mar 12. PubMed PMID: 25792236.

纯度：≥98%

CAS：1236109-67-3