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Bedaquiline fumarate

Cat. No. M6170
Bedaquiline fumarate Structure
Synonym:

R403323; TMC207 fumarate; R207910 fumarate

Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 280 In stock
50mg USD 900 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
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 Experiment
Animal models BALB/c mice
Formulation
Dosages 25 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 671.58
Formula C36H35BrN2O6
CAS Number 845533-86-0
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

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.

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Keywords: Bedaquiline fumarate, R403323; TMC207 fumarate; R207910 fumarate supplier, inhibitors

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