1140897-32-0
1140897-32-0 structure
- Name: BMS-823778 free base
- Chemical Name: Bms-823778 Free Base
- CAS Number: 1140897-32-0
- Molecular Formula: C18H18ClN3O
- Molecular Weight: 327.808
- Create Date: 2020-01-13 18:00:00
- Modify Date: 2024-01-20 17:30:50
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BMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2; exhibits robust acute pharmacodynamic effects in cynomolgus monkeys (ED50=0.6mg/Kg) and in diet-induced obese (DIO) mice (ED50=34 mg/Kg), also showed excellent inhibition in an ex vivo adipose DIO mouse model (ED50=5.2 mg/Kg). Diabetes Phase 2 Clinical
| Name | Bms-823778 Free Base |
|---|---|
| Synonyms |
Bms-823778 Free Base
2-{3-[1-(4-Chlorophenyl)cyclopropyl][1,2,4]triazolo[4,3-a]pyridin-8-yl}-2-propanol 1,2,4-Triazolo[4,3-a]pyridine-8-methanol, 3-[1-(4-chlorophenyl)cyclopropyl]-α,α-dimethyl- |
| Description | BMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2; exhibits robust acute pharmacodynamic effects in cynomolgus monkeys (ED50=0.6mg/Kg) and in diet-induced obese (DIO) mice (ED50=34 mg/Kg), also showed excellent inhibition in an ex vivo adipose DIO mouse model (ED50=5.2 mg/Kg). Diabetes Phase 2 Clinical |
|---|---|
| References | References 1. Cheng Y, et al. Br J Clin Pharmacol. 2018 Jan;84(1):130-141. 2. Jun Li, et al. Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1). ACS Med. Chem. Lett. 2018 Nov. DOI: 10.1021/acsmedchemlett.8b00307. View Related Products by Target 11β-HSD Diabetes |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C18H18ClN3O |
| Molecular Weight | 327.808 |
| Exact Mass | 327.113831 |
| LogP | 3.03 |
| Index of Refraction | 1.673 |