BM635是 MmpL3 的抑制剂, 具有出色的抗分歧杆菌活性。抑制结合分歧杆菌H37Rv的MIC50 值为0.12 μM。
Description | BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC50 of 0.12 μM against M. tuberculosis H37Rv. | ||||||||||||||||
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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 (IC95%: 43–54 mg/Kg)[1]. The half-life in vivo of BM635 is 1h, allowing a reasonable maximum concentration (Cmax=1.62 μM) and a moderate bioavailability (46%). Its poor aqueous solubility together with its high lipophilicity leads to low exposure in vivo[2]. | ||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : 31 mg/mL (78.98 mM; Need ultrasonic and warming) Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References |
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