1009583-20-3
1009583-20-3 structure
- Name: BMS-816336
- Chemical Name: BMS-816336
- CAS Number: 1009583-20-3
- Molecular Formula: C21H27NO3
- Molecular Weight: 341.44
- Catalog: Research Areas Metabolic Disease
- Create Date: 2019-03-30 17:19:34
- Modify Date: 2024-01-09 17:49:43
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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[1].
| Name | BMS-816336 |
|---|
| 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]. |
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| Related Catalog | |
| 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: An ED50 of 8.6 mg/kg and a plasma EC50 of 0.85 μM were calculated for 6n-2 in this model[1]. |
| References |
| Molecular Formula | C21H27NO3 |
|---|---|
| Molecular Weight | 341.44 |
| Storage condition | -20°C |