Product Overview
BMS-378806 is a novel attachment inhibitor of HIV with EC50 values of 2.68±1.64nM, 26.5±3.5nM, 2.94±2.01nM,15.5±6.8nM, 3.46±0.81nM, 1.47±0.63nM and 0.85±0.13nM for LAI(T), SF-2(T),NL4-3(T), Bal(M), SF-162(M), JRFL(M) and TLAV(dual), respectively. In a series of in vitro biochemical assay, BMS-378806 has been found to be not an effective inhibitor of HIV integrase, protease, or reverse transcriptase, but compete with soluble CD4 binding to a monomeric form of gp120 protein in an ELISA assay with an IC50 value of ~100nM. In addition, BMS-378806 has shown no overt cytotoxicity toward the host cell with a CC50 value of >225μM.
Chemical Name
1-[(2R)-4-benzoyl-2-methylpiperazin-1-yl]-2-(4-methoxy-1H-pyrrolo[2,3-b]pyridin-3-yl)ethane-1,2-dione