BMS-823778

• 常用名: BMS-823778
• 英文名: BMS-823778
• CAS号: 1140898-87-8
• 分子量: 364.269
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₈H₁₈ClN₃O·HCl
• 熔点: N/A
• 闪点: N/A

BMS-823778用途

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

BMS-823778名称

• 英文名: BMS823778

BMS-823778生物活性

• 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
• 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

BMS-823778物理化学性质

• 分子式: C₁₈H₁₈ClN₃O·HCl
• 分子量: 364.269
• 精确质量: 363.090515
• InChIKey: MQBBSMNIRWXALO-UHFFFAOYSA-N
• SMILES: CC(C)(O)c1cccn2c(C3(c4ccc(Cl)cc4)CC3)nnc12.Cl

BMS-823778靶点实验

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实验名称：Stability of the compound in hydrolytic solution 来源：ChEMBL 靶标：N/A External Id：CHEMBL4329732

实验名称：Stability of the compound in oxidative solution 来源：ChEMBL 靶标：N/A External Id：CHEMBL4329731

实验名称：Stability of the compound in solid state 来源：ChEMBL 靶标：N/A External Id：CHEMBL4329730

实验名称：Stability of the compound under high intensity light/UV light measured after 12 weeks... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4329729

实验名称：Stability of the compound at 50 degC measured after 12 weeks using crystalline solid ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4329728

实验名称：Stability of the compound in aqueous buffer at pH 1.1 to pH 7.4 at 40 degC measured a... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4329727

实验名称：Aqueous solubility of the compound at pH 1 using crystalline sample 来源：ChEMBL 靶标：N/A External Id：CHEMBL4329726

实验名称：Aqueous solubility of the compound at pH 6.5 using crystalline sample 来源：ChEMBL 靶标：N/A External Id：CHEMBL4329725

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BMS-823778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