1610562-74-7
Chemical Structure
BMS-986118
- CAS No.: 1610562-74-7
- Formula:C25H28ClF3N4O4
- Molecular Weight:540.96
IUPAC Name: 2-((4S,5S)-1-(4-(((3R,4R)-1-(5-chloro-2-methoxypyridin-4-yl)-3-methylpiperidin-4-yl)oxy)phenyl)-4-methyl-3-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-5-yl)acetic acid
InChIKey: GKIUHMMLGAMMOO-OITFXXTJSA-N
SMILES: COC1=CC(N2CC[C@H]([C@@H](C2)C)OC3=CC=C(C=C3)N4[C@H]([C@@H](C(C(F)(F)F)=N4)C)CC(O)=O)=C(C=N1)Cl
Biological Activity: BMS-986118 is an orally active and selective GPR40 full agonist (EC50 = 0.07 μM). BMS-986118 induces GLP-1 secretion and increases GLP-1 and insulin levels when combined with DPP-4 inhibitors. BMS-986118 shows sustained glucose-lowering effects. BMS-986118 can be used for research on type 2 diabetes[1][2][3][4][5][6][7].
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BMS-986118 | BMS-986118 is an orally active and selective GPR40 full agonist (EC50 = 0.07 μM). BMS-986118 induces GLP-1 secretion and increases GLP-1 and insulin levels when combined with DPP-4 inhibitors. BMS-986118 shows sustained glucose-lowering effects. BMS-986118 can be used for research on type 2 diabetes. | |||||||||||||||||||||
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References
- [1]. Shi J, et al. Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists. Journal of medicinal chemistry. 2018 Feb 08;61(3):681-694. [Content Brief]
- [2]. Chen HY, et al. Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs. ACS medicinal chemistry letters. 2018 Jul 12;9(7):685-690. [Content Brief]
- [3]. He J, et al. Small-molecule GLP-1 secretagogs: challenges and recent advances. Drug discovery today. 2020 Aug 21.
- [4]. Belete TM, et al. A Recent Achievement In the Discovery and Development of Novel Targets for the Treatment of Type-2 Diabetes Mellitus. Journal of experimental pharmacology. 2020;12:1-15.
- [5]. Li Z, et al. Free Fatty Acid Receptor 1 (FFAR1) as an Emerging Therapeutic Target for Type 2 Diabetes Mellitus: Recent Progress and Prevailing Challenges. Medicinal research reviews. 2018 Mar;38(2):381-425.
- [6]. Li Z, et al. Free fatty acid receptor agonists for the treatment of type 2 diabetes: drugs in preclinical to phase II clinical development. Expert opinion on investigational drugs. 2016 Aug;25(8):871-90.
- [7]. Eleazu C, et al. Free fatty acid receptor 1 as a novel therapeutic target for type 2 diabetes mellitus-current status. Chemico-biological interactions. 2018 Jun 01;289:32-39.
