Bedaquiline fumarate

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Chemical Structure| 845533-86-0 同义名 : R403323;TMC207 fumarate;TMC-207;R207910 fumarate
CAS号 : 845533-86-0
货号 : A648653
分子式 : C36H35BrN2O6
纯度 : 98%
分子量 : 671.577
MDL号 : MFCD28167761
存储条件:

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

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

动物实验配方:
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].
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 -
实验方案
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

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.