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Rifampicin

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Chemical Structure| 13292-46-1 同义名 : 利福平 ;Rifampin;Rifamycin AMP;Sinerdol;Fenampicin;Eremfat;Doloresum;Benemicin;Arzide;Arficin;Archidyn;Tubocin;Rimactan;Rimactane;Rifadin;NIH 10782;NSC-113926
CAS号 : 13292-46-1
货号 : A146981
分子式 : C43H58N4O12
纯度 : 98%
分子量 : 822.94
MDL号 : MFCD00151389
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(30.38 mM)，配合低频超声，并水浴加热至45℃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 Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. The steatogenic effect on the liver of Rifampicin, a potent inhibitor of the DNA-dependent RNA polymerase in bacteria. Fatty liver can be induced by very high doses of Rifampicin (400 mg/kg) in rats[3]. Rifampicin (30 mg/kg, i.p.) treatment of S464P biofilms in vivo results in a slight decline, but earlier rebinds in bioluminescence from these catheters compared with the parental signal, whereas rifampicin has no affect on bioluminescence in mice infected with mutant H481Y[4]. The antituberculosis drug rifampicin (rifampin) induces a number of drug-metabolising enzymes, having the greatest effects on the expression of cytochrome P450 (CYP) 3A4 in the liver and in the small intestine. In addition, rifampicin induces some drug transporter proteins, such as intestinal and hepatic P-glycoprotein[5]. Rifampicin (100 mg/mL) can block the functional activity of P-glycoprotein. Rifampicin is not a substract for P-glycoprotein. The mechanism of rifampicin resistance is unassociated with the functional activity of P-glycoprotein[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.22mL

0.24mL

0.12mL

6.08mL

1.22mL

0.61mL

12.15mL

2.43mL

1.22mL
参考文献

[1]Jean-Baptiste E, Blanchemain N, et al. Evaluation of the anti-infectious properties of polyester vascular prostheses functionalised with cyclodextrin. J Infect. 2014 Feb;68(2):116-24.

[2]Wang X, Grace PM, et al. Rifampin inhibits Toll-like receptor 4 signaling by targeting myeloid differentiation protein 2 and attenuates neuropathic pain. FASEB J. 2013 Jul;27(7):2713-22.

[3]Piriou A, Warnet JM, Jacqueson A, Claude JR, Truhaut R. Fatty liver induced by high doses of rifampicin in the rat: possible relation with an inhibition of RNA polymerases in eukariotic cells. Arch Toxicol Suppl. 1979;(2):333-7

[4]Yu J, Wu J, Francis KP, Purchio TF, Kadurugamuwa JL. Monitoring in vivo fitness of rifampicin-resistant Staphylococcus aureus mutants in a mouse biofilm infection model. J Antimicrob Chemother. 2005 Apr;55(4):528-34

[5]Niemi M, Backman JT, Fromm MF, Neuvonen PJ, Kivistö KT. Pharmacokinetic interactions with rifampicin : clinical relevance. Clin Pharmacokinet. 2003;42(9):819-50

[6]Erokhina MV, Aleksandrova EA. [In vitro development of rifampicin resistance in the epithelial cells]. Probl Tuberk Bolezn Legk. 2006;(8):58-61. Russian