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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Diglyceride Acyltransferase (DGAT)-BMS-986172
BMS-986172

Chemical Structure : BMS-986172

CAS No.: 1808258-99-2

BMS-986172 (BMS986172)

货号: PC-21221Not For Human Use, Lab Use Only.

BMS-986172 is a highly potent, selective monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with IC50 of 4.6 nM (human MGAT2).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BMS-986172 is a highly potent, selective monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with IC50 of 4.6 nM (human MGAT2).
BMS-986172 shows no activity against lipid acyltransferases including recombinant human DGAT1, DGAT2, MGAT1, AWAT1, AWAT2, DC3, ACAT1, and ACAT2 (all IC50 > 30 uM), MGAT3 (IC50=16 uM).
BMS-986172 shows excellent liver microsome and UGT metabolic stabilities, and no species-variable glucuronidation.
BMS-986172 (0.03, 0.1, 0.3, and 1.0 mg/kg) displays a statistically significant and dose-dependent reduction in food intake in DIO mice, reduces food intake and body weight in wild-type mice with a minimum efficacious dose of 0.1 mg/kg (5% weight loss).

物理化学性质&存储条件

分子量 589.47
分子式 C24H22F7N7O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-4-(1-(Cyclopropylmethyl)-1H-pyrazol-3-yl)-6-(2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl)-3-(5-oxo-4,5-dihydro-1H-tetrazol-1-yl)-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one

参考文献

1. Wei Meng, et al. J Med Chem. 2023 Sep 19. doi: 10.1021/acs.jmedchem.3c01147.

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