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.
Wilforine is a sesquiterpene pyridine alkaloid; important bioactive compound in T. wilfordii plants, and is effective in treating idiopathic pulmonary fibrosis.
Wilfortrine is an immunomodulatory compound isolated from Tripterygium wilfordii.
Etanercept is a dimeric fusion protein consisting of two ligand-binding domains of human p75 tumor necrosis factor receptor and the human IgG1 Fc portion.
Tocilizumab is a humanized monoclonal antibody that binds to the interleukin-6 receptor, MW: 148 KD.
Lambrolizumabis a potent, highly selective, fully humanized immunoglobulin (Ig) G4-kappa monoclonal antibody against PD-1 with potential immune checkpoint inhibitory and antineoplastic activities. MW : 146.286 KD.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.