tcsc0032638 BM635

BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC₅₀ of 0.12 μM against M. tuberculosis H37Rv.

IC50 & Target: MIC50: 0.12 μM (M. tuberculosis H37Rv)^[1]

In Vivo: BM635 has potent MIC (0.12 µM), Tox₅₀:MIC ratio of >100, and good microsomal stability in mice (1.4 mL/min/g). When tested in an acute murine infection model at multiple doses, BM635 exhibits potent anti-tubercular activity, with an ED₉₉ of 49 mg/Kg (IC_95%: 43–54 mg/Kg)^[1]. The half-life in vivo of BM635 is 1h, allowing a reasonable maximum concentration (C_max=1.62 μM) and a moderate bioavailability (46%). Its poor aqueous solubility together with its high lipophilicity leads to low exposure in vivo^[2].