英文名 | BMS823778 |
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英文别名 |
C82R061MZ5
BMS 823778 2-{3-[1-(4-Chlorophenyl)cyclopropyl][1,2,4]triazolo[4,3-a]pyridin-8-yl}-2-propanol hydrochloride (1:1) 3-[1-(4-Chlorophenyl)cyclopropyl]-α,α-dimethyl-1,2,4-triazolo[4,3-a]pyridine-8-methanol hydrochloride 1,2,4-Triazolo[4,3-a]pyridine-8-methanol, 3-[1-(4-chlorophenyl)cyclopropyl]-α,α-dimethyl-, hydrochloride (1:1) MFCD30718574 BMS823778 Bms-823778 BMS-823778-03 |
描述 | BMS-823778(BMS823778)是一种口服,有效和选择性的11βHSD-1抑制剂,IC50为2.3 nM,选择性比11βHSD-2高10,000倍;在食蟹猴中表现出强大的急性药效学作用(ED50=0.6mg/Kg)和饮食诱导的肥胖(DIO)小鼠(ED50=34mg/Kg)在离体也显示出优异的抑制作用脂肪DIO小鼠模型(ED50=5.2mg/Kg)。糖尿病2期临床 |
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参考文献 | References 1. Cheng Y, et al. Br J Clin Pharmacol. 2018 Jan;84(1):130-141. 2. Jun Li, et al. Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1). ACS Med. Chem. Lett. 2018 Nov. DOI: 10.1021/acsmedchemlett.8b00307. View Related Products by Target 11β-HSD Diabetes |
分子式 | C18H18ClN3O·HCl |
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分子量 | 364.269 |
精确质量 | 363.090515 |