BMS-823778 free base
Names
[ CAS No. ]:
1140897-32-0
[ Name ]:
BMS-823778 free base
[Synonym ]:
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-
Biological Activity
[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
Chemical & Physical Properties
[ 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