| 货号 | 14423-100mg |
| 描述 | Rifampicin is a member of the rifamycin class of antibiotics, as it inhibits bacterial DNA-dependent RNA synthesis (Ki = ~ 1 nM).1 While this compound does not directly affect RNA synthesis in humans, its use as an antibiotic is limited by its potency toward activation of the pregnane X receptor (PXR, EC50 = ~2 µM), which results in the up-regulation of enzymes that alter drug metabolism.2 Access of rifampicin to the nuclear receptor PXR requires its import into the cell via organic anion transporters (OATs) in the OAT polypeptide (OATP) family.3 By acting as a transporter substrate, rifampicin inhibits OATPs with Ki/IC50 values ranging from 0.58-18 µM.4,3,5,6 |
| 别名 | NIH 10782;NSC 113926;Rifampin; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Wehrli, W. Rifampin: Mechanisms of action and resistance. Rev.Infect.Dis. 5(3), S407-S411 (1983). 2.Gill, S.K.,Xu, H.,Kirchhoff, P.D., et al. Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. Journal of Medicinal Chemistry 55(8), 3814-3826 (2012). 3.Tirona, R.G.,Leake, B.F.,Wolkoff, A.W., et al. Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation. Journal of Pharmacology and Experimental Therapeutics 304(1), 23-228 (2003). 4.Shitara, Y.,Sugiyama, D.,Kusuhara, H., et al. Comparative inhibitory effects of different compounds on rat Oatp1 (Slc21a1)- and Oatp2 (Slc21a5)-mediated transport. Pharmaceutical Research 19(2), 147-153 (2002). 5.Karlgren, M.,Vildhede, A.,Norinder, U., et al. Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): Influence of protein expression on drug-drug interactions. Journal of Medicinal Chemistry 55(10), 4740-4763 (2012). 6.Izumi, S.,Nozaki, Y.,Komori, T., et al. Substrate-dependent inhibition of organic anion transporting polypeptide 1B1: Comparative analysis with prototypical probe substrates estradiol-17β-glucuronide, estrone-3-sulfate, and sulfobromophthalein. Drug Metabolism and Disposition 41(10), 1859-1866 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥90% |
| 计算分子量 | 823 |
| 分子式 | C43H58N4O12 |
| CAS号 | 13292-46-1 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |