BMS-986118 (CAS: 1610562-74-7 )
Background Information of BMS-986118
BMS-986118 is a potent and selective G protein-coupled receptor 40 (GPR40) agonist with an EC50 of 70 nM. GPR40, also known as free fatty acid receptor 1 (FFAR1), is a Gq protein-coupled receptor (GPCR) that is predominately expressed in pancreatic β-cells and is also found in the GI tract and brain. The constellation of GPR40-mediated effects makes it an attractive target for the treatment of type-2 diabetes.
Storage Condition of BMS-986118
Quality Control and Spectral Data
Mechanism and Indications
||Sponsor & Collaborators
Structure Information of BMS-986118
||C1C(Cl)=C(N2C[[email protected]@H](C)[[email protected]](OC3C=CC(N4N=C(C(F)(F)F)[[email protected]@H](C)[[email protected]@H]4CC(O)=O)=CC=3)CC2)C=C(OC)N=1 |&1:6,8,21,23|
Other Form Products of BMS-986118
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Recommended Products in the Same Indication
Safety Data of BMS-986118
Chemical and Physical Properties
||Solubility:Soluble in DMSO
.Shi J, et al. Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists. J Med Chem. 2018 Feb 8;61(3):681-694.
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and potent GPR40 agonists with a dual mechanism of action, promoting both glucose-dependent insulin and incretin secretion. Employing strategies to increase polarity and the ratio of sp3/sp2 character of the chemotype, we identified BMS-986118 (compound 4), which showed potent and selective GPR40 agonist activity in vitro. In vivo, compound 4 demonstrated insulinotropic efficacy and GLP-1 secretory effects resulting in improved glucose control in acute animal models.