Rifapentine是一种半合成的利福霉素类长效抗生素。
Cas No.:61379-65-5
Sample solution is provided at 25 µL, 10mM.
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Rifapentine is a semi-synthetic, long-acting rifamycin antibiotic. Rifapentine binds to the beta subunit of bacterial DNA-dependent RNA polymerase, thereby blocking the transcription process and exerting its bactericidal effect by inhibiting bacterial RNA synthesis. Rifapentine can be used in the research and treatment of tuberculosis (such as active pulmonary tuberculosis and latent tuberculosis infection), leprosy, and other infections caused by susceptible bacteria[1-4].
In vitro, Rifapentine (2.5μM) and Vincristine (5nM) were used to treat P-gp-overexpressing drug-resistant KBV20C cancer cells for 48 hours. Rifapentine significantly increased cytotoxicity but did not exhibit significant P-gp inhibitory activity[5]. Rifapentine (0.001-10μg/mL) was used to pretreat the human monocytic leukemia cell line (THP-1), followed by infection with the virulent NMI strain. Rifapentine significantly inhibited bacterial growth[6].
In vivo, administered via gavage either before or after infection, Rifapentine (20mg/kg/day) was given to wild-type and immunodeficient Yellow fever virus (YFV)-infected mice for 21 days. Rifapentine significantly improved the survival rate, alleviated clinical signs, and reduced the viral load and degree of injury in target organs[7]. Rifapentine (10mg/kg; once weekly) alone or in combination with Isoniazid and other drugs was administered to Swiss mice infected with Mycobacterium tuberculosis (M. tuberculosis H37Rv) for 6 months. Rifapentine monotherapy failed to clear the bacteria from the mouse lungs and selected for rifampicin-resistant mutants; the combination therapy with Moxifloxacin and other drugs significantly suppressed the lung bacterial load and reduced the relapse rate after discontinuation[8].
References:
[1] Sharma SK, Sharma A, Kadhiravan T, et al. Rifamycins (rifampicin, rifabutin and rifapentine) compared to isoniazid for preventing tuberculosis in HIV-negative people at risk of active TB. Cochrane Database Syst Rev. 2013 Jul 5;2013(7):CD007545.
[2] Klemens SP, Cynamon MH. Activity of rifapentine against Mycobacterium avium infection in beige mice. J Antimicrob Chemother. 1992 May;29(5):555-61.
[3] Albano M, Karau MJ, Greenwood-Quaintance KE, et al. In Vitro Activity of Rifampin, Rifabutin, Rifapentine, and Rifaximin against Planktonic and Biofilm States of Staphylococci Isolated from Periprosthetic Joint Infection. Antimicrob Agents Chemother. 2019 Oct 22;63(11):e00959-19.
[4] Rifat D, Prideaux B, Savic RM, et al. Pharmacokinetics of rifapentine and rifampin in a rabbit model of tuberculosis and correlation with clinical trial data. Sci Transl Med. 2018 Apr 4;10(435):eaai7786.
[5] Lee JS, Oh Y, Kim HS, et al. Low-Dose Rifabutin Increases Cytotoxicity in Antimitotic-Drug-Treated Resistant Cancer Cells by Exhibiting Strong P-gp-Inhibitory Activity. Int J Mol Sci. 2022 Jul 2;23(13):7383.
[6] Miller HK, Kersh GJ. Efficacy of rifapentine and other rifamycins against Coxiella burnetii in vitro. Microbiol Spectr. 2024 Jul 2;12(7):e0103424.
[7] Qian X, Wu B, Tang H, et al. Rifapentine is an entry and replication inhibitor against yellow fever virus both in vitro and in vivo. Emerg Microbes Infect. 2022 Dec;11(1):873-884.
[8] Lounis N, Bentoucha A, Truffot-Pernot C, et al. Effectiveness of once-weekly rifapentine and moxifloxacin regimens against Mycobacterium tuberculosis in mice. Antimicrob Agents Chemother. 2001 Dec;45(12):3482-6.
Rifapentine是一种半合成的利福霉素类长效抗生素。Rifapentine可与细菌DNA依赖性RNA聚合酶的 β 亚基结合，通过抑制细菌RNA的合成来阻断转录过程并发挥杀菌作用。Rifapentine可用于结核病（如活动性肺结核及潜伏性结核感染）、麻风病以及其他敏感菌所致感染的相关研究与治疗[1-4]。
在体外，Rifapentine（2.5μM）与Vincristine（5nM）处理P-gp过表达的耐药KBV20C癌细胞48小时。Rifapentine显著增加细胞毒性，同时未表现显著的P-gp抑制活性[5]。Rifapentine（0.001-10μg/mL）预处理人单核细胞白血病细胞系（THP-1），随后以virulent NMI菌株感染。Rifapentine显著抑制细菌的生长[6]。
在体内，在感染前或感染后通过灌胃给药，Rifapentine（20mg/kg/day）用于处理野生型及免疫缺陷的Yellow fever virus（YFV）感染小鼠，连续21天。Rifapentine显著提高了小鼠的存活率，减轻了临床体征，并降低了靶器官的病毒载量与损伤程度[7]。Rifapentine（10mg/kg；每周一次）单独或联合Isoniazid等药物持续6个月，用于处理感染结核分枝杆菌（M. tuberculosis H37Rv）的Swiss小鼠。Rifapentine单药治疗未能清除小鼠肺部细菌并筛选出利福平耐药突变株；与Moxifloxacin等药物的联合疗法则显著抑制了肺部细菌负荷并降低了停药后的复发率[8]。
| Cell experiment [1]: | |
Cell lines | P-gp-overexpressing drug-resistant KBV20C cancer cells |
Preparation Method | KBV20C cells were cultured and treated with Rifapentine (2.5μM) for 24 hours, either as a single agent or in combination with Vincristine (VIC). |
Reaction Conditions | 2.5μM; 24h |
Applications | Rifapentine exerted markedly lower cytotoxicity in VIC-co-treated KBV20C cells compared to rifabutin. Rifapentine exhibited minor P-gp-inhibitory activity and did not display sensitization effects on VIC-treated KBV20C cells. |
| Animal experiment [2]: | |
Animal models | type I interferon receptor knockout A129-/- and wild-type C57 mice |
Preparation Method | Mice were infected with Yellow fever virus (YFV) and administered Rifapentine by gavage either 24h prior to or post infection. Sofosbuvir was used as a control. Mice were sacrificed at day 4 post-infection for serum and tissue homogenate analysis. |
Dosage form | 20mg/kg/day; gavage; once daily for 21 days |
Applications | Rifapentine significantly improved the survival rate, alleviated clinical signs, and reduced virus load and injury in targeted organs of YFV-infected mice. Rifapentine reduced virus titres in serum, brain, and spleen, and mitigated inflammatory cell infiltration and organ damage. |
References: | |
| Cas No. | 61379-65-5 | SDF | |
| 别名 | 利福喷丁; DL 473; Cyclopentylrifampicin | ||
| Canonical SMILES | O[C@H]([C@H](C)[C@@H](O)[C@@H](C)/C=C/C=C1/C)[C@@H](C)[C@@](OC(C)=O)([H])[C@H](C)[C@@H](OC)/C=C/O[C@@]2(C)OC3=C(C2=O)C(C(O)=C4/C=N/N5CCN(C6CCCC6)CC5)=C(C(O)=C3C)C(O)=C4NC1=O | ||
| 分子式 | C47H64N4O12 | 分子量 | 877.03 |
| 溶解度 | ≥ 30.25mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1402 mL | 5.7011 mL | 11.4021 mL |
| 5 mM | 228 μL | 1.1402 mL | 2.2804 mL |
| 10 mM | 114 μL | 570.1 μL | 1.1402 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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