Bedaquiline fumarate | R403323;TMC207 fumarate;TMC-207;R207910 fumarate | ATP Synthase | Antibacterial

Bedaquiline fumarate/贝达喹啉富马酸盐 {[allProObj[0].p_purity_real_show]}

货号：A648653 同义名： R403323; TMC207 fumarate

Bedaquiline fumarate 是一种二芳基喹啉类抗生素，靶向 ATP 合成酶，对结核分枝杆菌具有抑制作用，适用于耐药性结核机制研究。

Bedaquiline fumarate/贝达喹啉富马酸盐化学结构
CAS号：845533-86-0

Bedaquiline fumarate/贝达喹啉富马酸盐 3D分子结构
CAS号：845533-86-0

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Bedaquiline fumarate/贝达喹啉富马酸盐生物活性

描述

Bedaquiline hinders the proliferation of TDR M. tuberculosis strains, showing MIC values within the range of 0.125 to 0.5 mg/LL^[1]. Bedaquiline demonstrates its highest efficacy against Mycobacterium avium among slowly growing mycobacteria (SGM), with MIC50 and MIC90 values of 0.03 and 16 mg/L, respectively. Among rapidly growing mycobacteria (RGM), both Mycobacterium abscessus subsp. abscessus (M. abscessus) and Mycobacterium abscessus subsp. massiliense (M. massiliense) appear to be more susceptible to bedaquiline compared to Mycobacterium fortuitum, with MIC50 and MIC90 values of 0.13 and >16 mg/L, respectively, for both species. Additionally, bedaquiline demonstrates moderate in vitro activity against non-tuberculous mycobacteria (NTM) species^[2]. Bedaquiline exhibits outstanding in vitro activity against Mycobacterium tuberculosis, including strains that are multidrug-resistant[3].

体外研究

Bedaquiline hinders the proliferation of TDR M. tuberculosis strains, showing MIC values within the range of 0.125 to 0.5 mg/LL^[1].

Bedaquiline demonstrates its highest efficacy against Mycobacterium avium among slowly growing mycobacteria (SGM), with MIC50 and MIC90 values of 0.03 and 16 mg/L, respectively. Among rapidly growing mycobacteria (RGM), both Mycobacterium abscessus subsp. abscessus (M. abscessus) and Mycobacterium abscessus subsp. massiliense (M. massiliense) appear to be more susceptible to bedaquiline compared to Mycobacterium fortuitum, with MIC50 and MIC90 values of 0.13 and >16 mg/L, respectively, for both species. Additionally, bedaquiline demonstrates moderate in vitro activity against non-tuberculous mycobacteria (NTM) species^[2].

Bedaquiline exhibits outstanding in vitro activity against Mycobacterium tuberculosis, including strains that are multidrug-resistant[3].

Bedaquiline fumarate/贝达喹啉富马酸盐细胞实验

Cell Line Mycobacterium avium Mycobacterium abscessus Mycobacterium abscessus Mycobacterium tuberculosis H37Rv Mycobacterium kansasii Mycobacterium abscessus subsp. massiliense Mycobacterium abscessus subsp. abscessus Mycobacterium intracellulare Mycobacterium avium Mycobacterium tuberculosis mutant CV37 Mycobacterium tuberculosis wild-type H37Rv Mycobacterium abscessus CIP104536T(S) THP-1 macrophages Mycobacterium abscessus CIP104536T	Concentration	Treated Time	Description	References
Mycobacterium avium	0.03 and 16 mg/L		Evaluate the in vitro activity of bedaquiline against nontuberculous mycobacteria, results showed that bedaquiline exhibited the highest activity against Mycobacterium avium	Antimicrob Agents Chemother. 2017 Apr 24;61(5):e02627-16.
Mycobacterium abscessus	0.5 μM (MIC)	48 h	To evaluate the effect of bedaquiline on the bactericidal activity of β-lactams. Results showed that bedaquiline dose-dependently reduced the bactericidal activity of β-lactams.	Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00827-19.
Mycobacterium abscessus	0.5 μM (MIC)	4 h	To determine whether β-lactams cause an increase in intrabacterial ATP and assess the inhibitory effect of bedaquiline on this burst. Results showed that β-lactams induced an ATP burst, which was suppressed by bedaquiline.	Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00827-19.
Mycobacterium tuberculosis H37Rv	0.5–1 µg/mL	14 days	To determine the minimum inhibitory concentration (MIC) of bedaquiline against Mycobacterium tuberculosis H37Rv. Results showed the MIC of bedaquiline was 0.5–1 µg/mL.	Antimicrob Agents Chemother. 2023 Dec 14;67(12):e0078923.
Mycobacterium kansasii	0.016 μg/ml		Evaluate the in vitro activity of Bedaquiline against nontuberculous mycobacteria, showing low MIC values for Mycobacterium kansasii.	Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00665-19.
Mycobacterium abscessus subsp. massiliense	0.062 μg/ml		Evaluate the in vitro activity of Bedaquiline against nontuberculous mycobacteria, showing low MIC values for Mycobacterium abscessus subsp. massiliense.	Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00665-19.
Mycobacterium abscessus subsp. abscessus	0.062 μg/ml		Evaluate the in vitro activity of Bedaquiline against nontuberculous mycobacteria, showing low MIC values for Mycobacterium abscessus subsp. abscessus.	Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00665-19.
Mycobacterium intracellulare	0.016 μg/ml		Evaluate the in vitro activity of Bedaquiline against nontuberculous mycobacteria, showing low MIC values for Mycobacterium intracellulare.	Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00665-19.
Mycobacterium avium	0.016 μg/ml		Evaluate the in vitro activity of Bedaquiline against nontuberculous mycobacteria, showing low MIC values for Mycobacterium avium.	Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00665-19.
Mycobacterium tuberculosis mutant CV37	0.06–0.0038 mg/L	4 weeks	To assess the selection advantage of Rv0678 mutants at sub-MIC concentrations, results showed significant enrichment of Rv0678 mutants at sub-MIC concentrations of BDQ and CFZ	Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0127523.
Mycobacterium tuberculosis wild-type H37Rv	0.06–0.0038 mg/L	4 weeks	To assess the selection advantage of Rv0678 mutants at sub-MIC concentrations, results showed significant enrichment of Rv0678 mutants at sub-MIC concentrations of BDQ and CFZ	Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0127523.
Mycobacterium abscessus CIP104536T(S)	0.125 μg/ml	4 days	To evaluate the in vitro growth inhibitory effect of bedaquiline on Mycobacterium abscessus, results showed that bedaquiline has a bacteriostatic effect against M. abscessus in vitro.	Antimicrob Agents Chemother. 2017 Oct 24;61(11):e01225-17.
THP-1 macrophages	20 µg/ml	2 days	To evaluate the therapeutic effect of VER and BDQ combination on M. abscessus-infected macrophages, results showed VER significantly enhanced BDQ activity	Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00705-19.
Mycobacterium abscessus CIP104536T	64 ng/ml	4 days	To determine the MIC of BDQ against M. abscessus, results showed VER significantly enhanced BDQ activity	Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00705-19.

Cell Line

Concentration

Treated Time

Description

References

Mycobacterium avium

0.03 and 16 mg/L

Evaluate the in vitro activity of bedaquiline against nontuberculous mycobacteria, results showed that bedaquiline exhibited the highest activity against Mycobacterium avium

Antimicrob Agents Chemother. 2017 Apr 24;61(5):e02627-16.

Mycobacterium abscessus

0.5 μM (MIC)

48 h

To evaluate the effect of bedaquiline on the bactericidal activity of β-lactams. Results showed that bedaquiline dose-dependently reduced the bactericidal activity of β-lactams.

Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00827-19.

Mycobacterium abscessus

0.5 μM (MIC)

4 h

To determine whether β-lactams cause an increase in intrabacterial ATP and assess the inhibitory effect of bedaquiline on this burst. Results showed that β-lactams induced an ATP burst, which was suppressed by bedaquiline.

Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00827-19.

Mycobacterium tuberculosis H37Rv

0.5–1 µg/mL

14 days

To determine the minimum inhibitory concentration (MIC) of bedaquiline against Mycobacterium tuberculosis H37Rv. Results showed the MIC of bedaquiline was 0.5–1 µg/mL.

Antimicrob Agents Chemother. 2023 Dec 14;67(12):e0078923.

Mycobacterium kansasii

0.016 μg/ml

Evaluate the in vitro activity of Bedaquiline against nontuberculous mycobacteria, showing low MIC values for Mycobacterium kansasii.