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1009583-20-3 | BMS-816336

BMS-816336 NLT 98%

SKU : MC501402

CAS Number : 1009583-20-3

Molecular Formula : C21H27NO3 | Molecular Weight : 341.44

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Purity NLT 98%
Storage at 20ºC 2 years
*The above information is for reference only.
Chemical Name BMS-816336
CAS Number 1009583-20-3
Molecular Formula C21H27NO3
Molecular Weight 341.44
Introduction of 1009583-20-3 :

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

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