Rifamycin  (Synonyms: 利福霉素钠; Rifamycin SV)

Rifamycin (Rifamycin SV) is an orally active ansamycin antibiotic. Rifamycin inhibits DNA-dependent RNA synthesis. Rifamycin has antibacterial activity against Mycobacterium tuberculosis. Rifamycin interferes with hepatic bile acid metabolism. Rifamycin has anti-inflammatory effects. Rifamycin can be used in the study of Mycobacterium tuberculosis, Bacteroides fragilis infection, and Lipopolysaccharide (HY-D1056B3)-induced inflammation^{[1][2][3][4][5][6][7][8][9][10][11]}.

Rifamycin (10 μM；30 s) 在短期培养的大鼠肝细胞中，主要抑制钠非依赖性 Taurocholate (HY-N0545) 摄取^[2]。
Rifamycin (10-100 μM；15 min) 在表达 Na⁺/Ntcp 的非洲爪蟾卵母细胞中，能有效抑制 Oatp2 介导的 Taurocholate 摄取^[2]。
Rifamycin (1-100 μM；24 h) 可抑制脂多糖激活的单核细胞和巨噬细胞合成细胞因子和趋化因子^[3]。
Rifamycin (0.16 μg/ml；培养 2 周) 在含 10% 血清白蛋白的 TB 肉汤培养基中，能抑制结核分枝杆菌 (M. tuberculosis) 及其耐药突变株的生长^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Rifamycin (5 mg/day；皮下注射；每周 3 天) 对感染结核分枝杆菌 (M. tuberculosis) 的小鼠有效，可显著降低其体内活菌数量^[4]。
Rifamycin (12.5-25 mg/kg；腹腔灌洗) 可提高实验性腹腔感染大鼠生存率，显著降低腹腔内细菌数量和粘连形成^[6]。
Rifamycin (5-40 mg/kg；食管给药；每天一次，每周 5 天；4 周) 可缩短溃疡分枝杆菌病小鼠模型的口服治疗时间^[8]。
Rifamycin (0.1 mL；经耳道给药；每天 2 次；10 天) 不会导致成年或断奶大鼠听力损失^[9]。
Rifamycin (静脉推注 1 mg，随后静脉输注 4 mg；70 min) 在大鼠静脉输注 Sodium cholate (HY-N0324A) 的动物模型中，会干扰肝脏胆汁酸代谢的三个主要步骤，导致胆汁酸摄取和排泄显著减少^[10]。
Rifamycin (10-160 mg/kg；皮下注射；单次) 在小鼠脆弱拟杆菌大腿感染模型中，疗效比 Metronidazole (HY-B0318) 低约 11 倍^[11]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

697.77

C₃₇H₄₇NO₁₂

6998-60-3

利福霉素

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Floss HG, et al. Rifamycin-mode of action, resistance, and biosynthesis. Chem Rev. 2005 Feb;105(2):621-32.  [Content Brief]

  [2]. Fattinger K, et al. Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2. Hepatology. 2000 Jul;32(1):82-6.  [Content Brief]

  [3]. Rosette C, et al. Anti-inflammatory and immunomodulatory activities of rifamycin SV. Int J Antimicrob Agents. 2013 Aug;42(2):182-6.  [Content Brief]

  [4]. Tsukamura M, et al. Antituberculous Action of Rifamycin SV* In Vitro and In Vivo Studies. The Journal of Antibiotics, Series A, 1962, 15(5): 216-224.

  [5]. Saito K, et al. Rifamycin action on RNA polymerase in antibiotic-tolerant Mycobacterium tuberculosis results in differentially detectable populations. Proc Natl Acad Sci U S A. 2017 Jun 13;114(24):E4832-E4840.  [Content Brief]

  [6]. Jallouli M, et al. Rifamycin lavage in the treatment of experimental intra-abdominal infection. J Surg Res. 2009 Aug;155(2):191-4.  [Content Brief]

  [7]. Zhang M, et al. Treatment of tuberculosis with rifamycin-containing regimens in immune-deficient mice. Am J Respir Crit Care Med. 2011 May 1;183(9):1254-61.  [Content Brief]

  [8]. Omansen TF, et al. High-Dose Rifamycins Enable Shorter Oral Treatment in a Murine Model of Mycobacterium ulcerans Disease. Antimicrob Agents Chemother. 2019 Jan 29;63(2):e01478-18.  [Content Brief]

  [9]. Özbay C, et al. Ototoxic effect of topical rifamycin SV applied in the middle ear of rats. The Turkish Journal of Ear Nose and Throat, 2017, 27(1): 31-38.

  [10]. Okolicsanyi L, et al. Influence of rifamycin SV on bile acid metabolism in rats. Naunyn Schmiedebergs Arch Pharmacol. 1980 Aug;313(2):171-4.  [Content Brief]

  [11]. Dijkmans B A C, et al. Efficacy of rifamycin SV and vancomycin against Bacteroides fragilis in vitro and in experimentally infected mice. Current Microbiology, 1985, 12: 53-58.