Bedaquiline inhibits the growth of TDR M. tuberculosis strains, with MIC values ranging from 0.125 to 0.5 mg/L. Among slowly growing mycobacteria (SGM), bedaquiline exhibits the highest activity against Mycobacterium avium with MIC50 and MIC90 values of 0.03 and 16 mg/L, respectively. Among rapidly growing mycobacteria (RGM), Mycobacterium abscessus subsp. abscessus (M. abscessus) and Mycobacterium abscessus subsp. massiliense (M. massiliense) seem more susceptible to bedaquiline than Mycobacterium fortuitum, with MIC50 and MIC90 values of 0.13 and >16 mg/L, respectively, for both species. Bedaquiline also shows moderate in vitro activity against NTM species. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis.
|Cell lines||M. tuberculosis|
|Preparation method||M. tuberculosis was cultured in 7H9 broth and grown to an A600 nm of 0.8. Cultures were treated with 0.1, 1 or 10 mg ml 1 BDQ for 24 h. NADH and NAD þ concentrations were determined and the NADH/NAD þ ratio was calculated as described.|
|Concentrations||0.1, 1 and 10 mg/ml|
|Incubation time||24 h|
|Animal models||BALB/c mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Verapamil increases the bactericidal activity of bedaquiline against Mycobacterium tuberculosis in a mouse model.
Gupta S, et al. Antimicrob Agents Chemother. 2015 Jan;59(1):673-6. PMID: 25331694.
Delayed bactericidal response of Mycobacterium tuberculosis to bedaquiline involves remodelling of bacterial metabolism
A Koul, et al. Nat Commun. 2014 Feb 26;5:3369. PMID: 24569628.
CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.
YM 511 is a potent aromatase (CYP19) inhibitor.
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YM 298198 hydrochloride is a highly potent, selective non-competitive mGlu 1 antagonist.
YM 022 is a highly potent, selective non-peptide CCK 2 antagonist.
YK 3-237 is a sIRT1 activator.
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