BMS-816336,1009583-20-3

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BMS-816336

CAS No. : 1009583-20-3

MCE 国际站：BMS-816336

产品活性：BMS-816336 是一种新型， 有效， 可口服的人 11β-羟基类固醇脱氢酶 1 型 (11β-HSD1) 抑制剂，IC₅₀ 为 3.0 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：11β-HSD

In Vitro: 11β-HSD1 inhibition may be useful in the treatment of type II diabetes and other potential clinical utilities such as atheroprotection and cognitive protection. BMS-816336 (6n-2) inhibits 11β-HSD1 enzyme in HEK and 3T3L1 cells with IC₅₀s of 37.3 and 28.6 nM, respectively.

In Vivo: BMS-816336 represents a potential new treatment for type 2 diabetes, metabolic syndrome, and other human diseases modulated by glucocorticoid control. BMS-816336 (6n-2) exhibits a robust acute pharmacodynamic effect in cynomolgus monkeys (ED₅₀=0.12 mg/kg) and in DIO mice (1, 3, 10, 30, 100 mg/kg, 120 mintues). It is orally bioavailable (%F ranges from 20 to 72% in preclinical species) and has a predicted pharmacokinetic profile of a high peak to trough ratio and short half-life in humans.

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