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BMS-816336
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-816336图片
CAS NO:1009583-20-3
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

产品介绍

产品描述

BMS-816336 is a novel, orally bioavailable inhibitor, and potent against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM[1].

体外活性

BMS-816336 (6n-2) inhibits 11β-HSD1 enzyme in HEK and 3T3L1 cells with IC50s of 37.3 and 28.6 nM, respectively. 11β-HSD1 inhibition may be useful in the treatment of type II diabetes and other potential clinical utilities such as atheroprotection and cognitive protection.[1].

体内活性

BMS-816336 represents a potential new treatment for type 2 diabetes, metabolic syndrome, and other human diseases modulated by glucocorticoid control. 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[1]. 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).

Cas No.

1009583-20-3

分子式

C21H27NO3

分子量

341.44

储存和溶解度

DMSO:300 mg/mL (878.63 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years