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BMS-816336 

Cat. No.: HY-101930
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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.

For research use only. We do not sell to patients.

BMS-816336 Chemical Structure

BMS-816336 Chemical Structure

CAS No. : 1009583-20-3

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Description

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].

Animal Model: Nonfasting diet-induced obese male mice[1]
Dosage: 1, 3, 10, 30, 100 mg/kg
Administration: Oral, 120 mintues
Result: ED50=8.6 mg/kg and a plasma EC50 of 0.85 μM in this model[1].
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

341.44

Formula

C₂₁H₂₇NO₃

CAS No.

1009583-20-3

SMILES
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BMS-816336
Cat. No.:
HY-101930
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BMS-816336

Cat. No.: HY-101930