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Bedaquiline

Cat. No. M9186
Bedaquiline Structure
Synonym:

R403323; TMC207; R207910

Size Price Availability Quantity
10mM*1mL in DMSO USD 70  USD70 In stock
5mg USD 60  USD60 In stock
10mg USD 85  USD85 In stock
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Quality Control & Documentation
Biological Activity

Bedaquiline (TMC207), a diarylquinoline antibiotic that targets ATP synthase, can be used for the research of Mycobacterium tuberculosis infections. 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.

Chemical Information
Molecular Weight 555.50
Formula C32H31BrN2O2
CAS Number 843663-66-1
Solubility (25°C) DMSO 10 mg/mL (Need ultrasonic and warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Jang JC, et al. J Microbiol. Bedaquiline susceptibility test for totally drug-resistant tuberculosis Mycobacterium tuberculosis.

[2] Chahine EB, et al. Ann Pharmacother. Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis.

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Keywords: Bedaquiline, R403323; TMC207; R207910 supplier, Antibiotic, inhibitors, activators


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