Catalog No.: PC-35792Not For Human Use, Lab Use Only.
BMS-823778 (BMS823778) freebase 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.
BMS-823778 (BMS823778) freebase 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.
BMS-823778 exhibits robust acute pharmacodynamic effects in cynomolgus monkeys (ED50=0.6mg/Kg) and in diet-induced obese (DIO) mice (ED50=34 mg/Kg).
BMS-823778 also showed excellent inhibition in an ex vivo adipose DIO mouse model (ED50=5.2 mg/Kg).
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.
