LKT Labs

Biochemicals for Life Science Research

Bedaquiline Fumarate

Product ID B165121
Cas No. 845533-86-0
Purity ≥98%
Product Unit SizeCostQuantityStock
5 mg $176.60 In stock
25 mg $529.70 In stock
100 mg $1,174.80 In stock
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Description

Bedaquiline is a diarylquinoline found to be useful in treating multidrug-resistant tuberculosis. In mouse models of TB, bedaquiline has significantly shortened the treatment regimen. A long-acting injectable formulation has been shown to have prolonged bactericidal activity.
Bedaquiline inhibits ATP-synthase, and at high concentrations leads to suppression of oxidative phosphorylation. In rat liver mitochondria, bedaquiline suppresses the formation of MPT pores, which typically accompanies the development of tuberculosis. Several analogues of bedaquiline that may improve its bioavailability are also in development.

Product Info

Cas No.

845533-86-0
Purity

≥98%
Formula

C36H35BrN2O6
Formula Wt.

671.59
Chemical Name

(1R,2S)-1-(6-Bromo-2-methoxy-3-quinolinyl)-4-(dimethylamino)-2-(1-naphthyl)-1-phenyl-2-butanol (2E)-2-butenedioate (1:1)
IUPAC Name

(1R,2S)-1-(6-Bromo-2-methoxy-3-quinolinyl)-4-(dimethylamino)-2-(1-naphthyl)-1-phenyl-2-butanol (2E)-2-butenedioate (1:1)
Synonym

Sirturo
Appearance

White to off-white powder

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

MSDS

B165121 MSDS PDF
Info Sheet

B165121 Info Sheet PDF

References

Sarathy J, Ganapathy U, Zimmerman M, et al. TBAJ-876, a 3,5-dialkoxypyridine analogue of bedaquiline, is active against mycobacterium abscessus. Antimicrob Agents Chemother. 2020 Mar 24;64(4):e02404-19. PMID: 31964791.

Xu J, Li SY, Almeida D, et al. Contribution of pretomanid to novel regimens containing bedaquiline with either linezolid or moxifloxacin and pyrazinamide in murine models of tuberculosis. Antimicrob Agents Chemother. 2019 Apr 25;63(5):e00021-19. PMID: 30833432.

Kaushik A, Ammerman N, Tyagi S, et al. Activity of a long-acting injectable bedaquiline formulation in a paucibacillary mouse model of latent tuberculosis infection. Antimicrob Agents Chemother. 2019 Mar 27;63(4):e00007-19. PMID: 30745396.

Belosludtsev K, Belosludtseva N, Talanov E, et al. Effect of bedaquilinr on the functions of rat liver mitochondria. Biochim Biophys Acta Biomembr. 2019 Jan;1861(1):288-297. PMID: 29920239.

Blaser A, Sutherland H, Tong A, et al. Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline. Bioorg Med Chem. 2019 Apr 1;27(7):1283-1291. PMID: 30792104.

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