BMS-823778

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BMS-823778 (BMS823778) 是一种口服有效的选择性 11βHSD-1 抑制剂，IC50 为 2.3 nM。

BMS-823778 (BMS823778) 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;?exhibits robust acute pharmacodynamic effects in cynomolgus monkeys (ED50=0.6mg/Kg) and in diet-induced obese (DIO) mice (ED50=34 mg/Kg), also showed excellent inhibition in an ex vivo adipose DIO mouse model (ED50=5.2 mg/Kg).Diabetes Phase 2 Clinical.

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Animal Model:Diet-induced obese (DIO) miceDosage:10-100 mg/kg Administration:Oral, once Result:Inhibition of 11β-HSD-1 was observed as a measure of decrease in the plasma concentration of corticosterone. The ED50 was 34 mg/kg.Animal Model:Male Balb/C mice Dosage:5 or 10 mg/kg Administration:IV or PO (Pharmacokinetic Analysis)Result:Single-Dose Pharmacokinetic Parameters of BMS-823778.

BMS823778

Metabolic Enzyme/Protease

11β-HSD

11β-HSD

Metabolic Disease

Diabetes

1140898-87-8

364.27

C18H18ClN3O · HCl

>98% (HPLC)

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CC(C)(C1=CC=CN2C1=NN=C2C3(CC3)C4=CC=C(C=C4)Cl)O.Cl

3-[1-(4-Chlorophenyl)cyclopropyl]-α,α-dimethyl-1,2,4-triazolo[4,3-a]pyridine-8-methanol hydrochloride

(-20℃)

With Ice Pack

≥ 2 years