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

货号:A648653 同义名: R403323;TMC207 fumarate

Bedaquiline fumarate, a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections.

Bedaquiline fumarate 化学结构 CAS号:845533-86-0
Bedaquiline fumarate 化学结构
CAS号:845533-86-0
Bedaquiline fumarate 3D分子结构
CAS号:845533-86-0
Bedaquiline fumarate 化学结构 CAS号:845533-86-0
Bedaquiline fumarate 3D分子结构 CAS号:845533-86-0
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Bedaquiline fumarate 纯度/质量文件 产品仅供科研

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Bedaquiline fumarate 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 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03625739 - Recruiting December 31, 2026 China ... 展开 >> Beijing Children's Hospital of Capital Medical University Recruiting Beijing, China Contact: Adong Shen, Master    13370115087    shenad16@hotmail.com 收起 <<
NCT03474198 Tuberculosis, Pulmonary Phase 2 Phase 3 Recruiting March 12, 2022 Philippines ... 展开 >> De La Salle Health Sciences Institute Not yet recruiting Manila, Philippines Lung Center Philippines Recruiting Manila, Philippines Philippines Tuberculosis Society Incorporated (PTSI) Not yet recruiting Manila, Philippines Tropical Disease Foundation Not yet recruiting Manila, Philippines Singapore National University Hospital Not yet recruiting Singapore, Singapore Thailand King Chulalongkorn Memorial Hospital Not yet recruiting Bangkok, Thailand 收起 <<
NCT00042289 HIV Infections Phase 4 Recruiting September 30, 2019 -

Bedaquiline fumarate 参考文献

[1]Ye X, et al. The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening. Bioorg Med Chem Lett. 2019 Feb 15;29(4):638-645.

[2]Chen X, et al. Targeting WD Repeat-Containing Protein 5 (WDR5): A Medicinal Chemistry Perspective. J Med Chem. 2021 Aug 12;64(15):10537-10556.

Bedaquiline fumarate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.49mL

0.30mL

0.15mL

7.45mL

1.49mL

0.74mL

14.89mL

2.98mL

1.49mL

Bedaquiline fumarate 技术信息

CAS号845533-86-0
分子式C36H35BrN2O6
分子量 671.577
别名 R403323;TMC207 fumarate;TMC-207;R207910 fumarate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 105 mg/mL(156.35 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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