利福喷丁 T1629

Product Introduction
Bioactivity


英文名: Rifapentine

描述: Rifapentine (Rifapentinum) 是可用于肺结核的抗生素。

体外活性: Rifapentine inhibits the function of DNA-dependent RNA polymerase in strains of M. tuberculosis, while inducing no effect on mammalian cells. Both Rifapentine and its active metabolite, 25-desacetylrifapentine, localize within monocyte-derived macrophages, thus allowing for intracellular inhibition of M. tuberculosis at a greater kill rate as compared with that of the parent or metabolite alone. Rifapentine is deacetylated in the liver and induces cytochrome P450 much less than rifampin. [1] Rifapentine has shown higher bacteriostatic and bactericidal activities (MICs and MBCs) than RMP, especially against intracellular bacteria growing in human monocyte-derived macrophages. [2]

体内活性: Rifapentine inhibits bacterial RNA synthesis by binding to the β-subunit of DNA-dependent RNA polymerase in susceptible species. Rifapentine is generally more active than rifampicin against sensitive strains of M. tuberculosis. [3] Rifapentine significantly increases the rate of antipyrine and pentobarbital metabolism in vivo. Rifapentine also increases liver weight, the content of liver microsomal protein and cytochrome P-450, the activity of NADPH-cytochrome C reductase and NADPH oxidase. [4] Rifapentine combined with isoniazid (INH) and pyrazinamide (PZA) administered daily results in an apparent clearance of M.tuberculosis organisms in the lungs and spleens of infected mice after 10 weeks of treatment. [5]

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

溶解度: DMSO : 93 mg/mL (106 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 14 mg/mL (16 mM)


关键字: inhibit | Rifapentine | DL473 | Bacterial | Inhibitor | MDL 473 | Antibiotic | MDL-473 | DL-473

相关产品: 360A | BCH001 | Norathyriol | α-​Chaconine | NSAH | ART558 | Saccharin 1-methylimidazole | Folinic acid calcium | Enoxacin | CeMMEC13

相关库: Drug Repurposing Compound Library | Antibiotics Library | Drug-induced Liver Injury (DILI) Compound Library | Toxic Compound Library | Anti-Cancer Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Macrocyclic Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug 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