BMS-823778 free base |CAS:1140897-32-0 Probechem Biochemicals

Chemical Structure : BMS-823778 free base

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BMS-823778 free base (BMS823778 )

货号: PC-35792Not For Human Use, Lab Use Only.

BMS-823778 (BMS823778) freebase is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2.

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生物&药学活性

BMS-823778 (BMS823778) freebase is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2.
BMS-823778 exhibits robust acute pharmacodynamic effects in cynomolgus monkeys (ED50=0.6mg/Kg) and in diet-induced obese (DIO) mice (ED50=34 mg/Kg).
BMS-823778 also showed excellent inhibition in an ex vivo adipose DIO mouse model (ED50=5.2 mg/Kg).

物理化学性质&存储条件

分子量	327.812
分子式	C18H18ClN3O
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	2-(3-(1-(4-chlorophenyl)cyclopropyl)-[1,2,4]triazolo[4,3-a]pyridin-8-yl)propan-2-ol

参考文献

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.

BMS-823778 free base (BMS823778 )

生物&药学活性

物理化学性质&存储条件

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BMS-823778 free base (BMS823778 )

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物理化学性质&存储条件

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