product name Rifapentine
Description: Rifapentine (also known as MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis. 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.
References: Ann Pharmacother. 1999 Nov;33(11):1203-10; Antimicrob Agents Chemother. 1995 Sep;39(9):2073-7; Drugs. 1998 Oct;56(4):607-16; discussion 617.
877.03
Formula
C47H64N4O12
CAS No.
61379-65-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (114.0 mM)
Water: <1 mg/mL
Ethanol: 17 mg/mL (19.4 mM)
Solubility (In vivo)
Synonyms
MDL473
other peoduct :
| In Vitro |
In vitro activity: The activities of rifampin and rifapentine against Mycobacterium tuberculosis residing in human monocytederived macrophages were determined. The MIC and MBC of rifapentine for intracellular bacteria were two- to four-fold lower than those of rifampin. For extracellular bacteria, this difference was less noticeable. Kinase Assay: Cell Assay: 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. Rifapentine has shown higher bacteriostatic and bactericidal activities (MICs and MBCs) than RMP, especially against intracellular bacteria growing in human monocyte-derived macrophages. |
|---|---|
| In Vivo | 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. 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. 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 |
| Animal model | |
| Formulation & Dosage | |
| References | Ann Pharmacother. 1999 Nov;33(11):1203-10; Antimicrob Agents Chemother. 1995 Sep;39(9):2073-7; Drugs. 1998 Oct;56(4):607-16; discussion 617. |
