化合物BTZ043 Racemate T6425

Product Introduction
Bioactivity


英文名: BTZ043 Racemate

描述: BTZ043 Racemate (Benzothiazinone 10526038) 是一种癸二烯基磷酰-β-D-核糖 2'-差向异构酶(DprE1) 抑制剂，用作新的抗分枝杆菌剂。

体外活性: By targeting decaprenylphosphoryl-β-D-ribose 2'-epimerase, BTZ043 abolishes the formation of decaprenylphosphoryl arabinose, leading to cell lysis and death of Mycobacterium tuberculosis. BTZ043 displays similar activity against all clinical isolates of M. tuberculosis, including multidrug-resistant and extensively drug-resistant strains. BTZ043 displays significant activity against M. tuberculosis H37Rv and Mycobacterium smegmatis with MIC of 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively, which is more potent than those of the existing tuberculosis (TB) drugs isoniazid (INH) and ethambutol (EMB) with MIC of 0.02-0.2 μg/mL and 1-5 μg/mL, respectively. BTZ043 is less effective in two different model systems (auxotrophy and starvation) involving metabolically inert M. tuberculosis, indicating that BTZ043 blocks a step in active metabolism similar to isoniazid (INH). BTZ043 treatment in M. smegmatis cells decreases the growth rate rapidly followed by a swelling of the poles and lysis of the cells after a few hours, which is similar but delayed in M. tuberculosis. [1] BTZ043 (1/4 MIC 0.375 ng/mL) in combination with TMC207 (1/4 MIC 20 ng/mL) has a stronger cidal effect on M. tuberculosis but not BTZ-resistant M. tuberculosis mutant than TMC207 alone at a concentration of 80 ng/mL. [2]

体内活性: In a mouse model of chronic tuberculosis, administration of BTZ043 at 37.5 mg/kg or 300 mg/kg for 4 weeks reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 21 mg/mL (48.7 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Benzothiazinone10526038 | inhibit | Benzothiazinone-10526038 | BTZ-044 | Inhibitor | BTZ-043 Racemate | BTZ-043 | BTZ-10526038 | BTZ043 | BTZ 043 | BTZ043 Racemate | tuberculosis | BTZ 10526038 | BTZ 044 | Bacterial

相关产品: Biapenem | Halazone | Sulfasalazine | 8-Hydroxyquinoline hemisulfate | Mecillinam | Clofoctol | Rimonabant hydrochloride | Netilmicin sulfate | Nigericin sodium salt | Dusquetide aceate

相关库: Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Inhibitor Library | Anti-Bacterial Compound Library | Preclinical Compound Library | NO PAINS Compound Library | Anti-Infection Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途