货号:A444634
同义名:
DL 473; Cyclopentylrifampicin
Rifapentine 是一种通过抑制 DNA 依赖性 RNA 聚合酶发挥作用的抗菌化合物,常被用于结核病的研究。


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| 产品名称 | DNA synthesis ↓ ↑ | helicase ↓ ↑ | RdRp ↓ ↑ | ribonucleotide reductase ↓ ↑ | tRNA synthetase ↓ ↑ | YB-1 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Fexinidazole | ✔ | 98% | |||||||||||||||||
| Daptomycin | ✔ | 98% | |||||||||||||||||
| Blasticidin S·HCl | ✔ | 98% | |||||||||||||||||
| Metronidazole | ✔ | 98% | |||||||||||||||||
| Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
| Triglycidyl isocyanurate | ✔ | p53 | 98+% | ||||||||||||||||
| Nedaplatin | ✔ | 99%+ | |||||||||||||||||
| Oxolinic acid | ✔ | 98+% | |||||||||||||||||
| Bendamustine | ✔ | 98+% | |||||||||||||||||
| Trifluridine | ✔ | 98% | |||||||||||||||||
| Robinetin | ✔ | 99%+ | |||||||||||||||||
| Carboplatin | ✔ | 99% | |||||||||||||||||
| Cidofovir | ✔ | 99% | |||||||||||||||||
| Cisplatin | ✔ | 99% | |||||||||||||||||
| Cytarabine |
++++
DNA synthesis, IC50: 16 nM |
98% | |||||||||||||||||
| Acelarin |
++++
DNA synthesis, EC50: 0.2 nM |
99%+ | |||||||||||||||||
| Oxaliplatin | ✔ | 98% | |||||||||||||||||
| YK-4-279 | ✔ | 99%+ | |||||||||||||||||
| ML216 |
+
BLMfull-length, IC50: 2.98 μM BLM636-1298, IC50: 0.97 μM |
99%+ | |||||||||||||||||
| RK-33 | ✔ | 98% | |||||||||||||||||
| Brr2-IN-3 | ✔ | 99%+ | |||||||||||||||||
| Phen-DC3 Trifluoromethanesulfonate | ✔ | 95% | |||||||||||||||||
| Favipiravir | ✔ | 99% | |||||||||||||||||
| Suramin sodium salt |
++
RdRp, IC50: 0.26 μM |
99%+ | |||||||||||||||||
| Clofarabine |
++
Ribonucleotide reductase, IC50: 65 nM |
97% | |||||||||||||||||
| Didox | ✔ | 98% | |||||||||||||||||
| (E)-3-AP | ✔ | 99% | |||||||||||||||||
| Halofuginone |
+++
prolyl-tRNA synthetase, Ki: 18.3nM |
99%+ | |||||||||||||||||
| BC-LI-0186 |
+++
Leucyl-tRNA synthetase, Kd: 42.1 nM Leucyl-tRNA synthetase, IC50: 46.11 nM |
98% | |||||||||||||||||
| SU056 |
+
YB-1, IC50: 1.73 μM |
98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Rifapentine is an antibiotic compound used in the treatment of tuberculosis. Antibacterial Rifapentine inhibits DNA-dependent RNA polymerase activity in susceptible cells. Specifically, it interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme[3]. The 3-month isoniazid-rifapentine regimen is as safe and effective as other recommended latent tuberculosis infection regimens and achieves significantly higher treatment completion rates[4]. Indeed, rifapentine too may decrease blood levels of many oral antidiabetics and compete with them for protein-binding sites and/or transporters. Rifapentine seems to be more suitable for use in diabetes patients with renal impairment, owing to the fact that it does not cause renal toxicity, and it is eliminated via kidneys in smaller proportions than rifampicin[5]. Rifapentine can be administered twice weekly during the intensive phase of tuberculosis treatment and then once weekly during the continuation phase of treatment. Rifapentine is well tolerated, with most patients experiencing adverse effects at a similar rate as rifampin[6]. |
| Concentration | Treated Time | Description | References | |
| Murine macrophages (J774 A.1) | 0, 5, 25, 50 μg/mL | 24 hours | Evaluate the cytotoxicity of nanoparticles, results showed nanoparticles were non-toxic to macrophages with cell viability over 90%. | Int J Nanomedicine. 2020 Oct 6;15:7491-7507. |
| Huh7 cells | 0.5259 µM | 48 hours | Evaluate the inhibitory effect of rifapentine on YFV, results showed that rifapentine significantly inhibited YFV infection | Emerg Microbes Infect. 2022 Dec;11(1):873-884. |
| A-498 cells | 0.01 µg/mL | 7 days | To evaluate the inhibitory effect of rifapentine on Coxiella burnetii, results showed that rifapentine exhibited significant inhibitory effects in A-498 cells with an MIC of 0.01 µg mL−1. | Microbiol Spectr. 2024 Jul 2;12(7):e0103424. |
| THP-1 cells | ≤0.01 µg/mL | 7 days | To evaluate the inhibitory effect of rifapentine on Coxiella burnetii, results showed that rifapentine exhibited significant inhibitory effects in THP-1 cells with an MIC ≤0.01 µg mL−1. | Microbiol Spectr. 2024 Jul 2;12(7):e0103424. |
| Mycobacterium tuberculosis | 0.03 to 0.25 mg/L | Evaluate the antimicrobial efficacy of rifapentine against M. tuberculosis, showing it is 2 to 10 times more potent than Rifampin | Front Pharmacol. 2025 Jan 17;15:1463575. |
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c mice | Latent tuberculosis infection model | Gavage | 15 mg/kg | Once weekly for 3 months | To evaluate the efficacy of rifapentine combined with isoniazid or moxifloxacin for the treatment of latent tuberculosis infection, showing that 3-month once-weekly rifapentine-containing regimens were as active as 6-9 months of daily isoniazid | Am J Respir Crit Care Med. 2005 Dec 1;172(11):1452-6 |
| Mice | Tuberculosis model | Oral | 15 mg/kg | Once weekly for 4 months | To evaluate the sterilizing activity of rifapentine in combination with moxifloxacin, results showed that once-weekly moxifloxacin plus rifapentine (15 mg/kg) was significantly more active than the predominantly twice-weekly Denver regimen | Am J Respir Crit Care Med. 2005 Dec 1;172(11):1457-62 |
| BALB/c mice | Murine model of tuberculosis | Oral | 15 or 20 mg/kg | Twice weekly for 4, 5, or 6 months | To evaluate the bactericidal and sterilizing activities of rifapentine in tuberculosis treatment, results showed that twice-weekly rifapentine (15 or 20 mg/kg) regimens were more effective than standard daily therapy, achieving stable cure within 4 months. | Am J Respir Crit Care Med. 2006 Jul 1;174(1):94-101 |
| A129−/− mice | YFV infection model | Gavage | 20 mg/kg/day | Once daily for 21 days | Evaluate the antiviral effect of rifapentine in YFV-infected mouse model, results showed that rifapentine significantly improved survival rate, alleviated clinical signs, and reduced virus load and injury in targeted organs | Emerg Microbes Infect. 2022 Dec;11(1):873-884. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02099240 | Osteomyelitis | Early Phase 1 | Recruiting | September 2019 | United States, Kentucky ... 展开 >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu Sub-Investigator: Forest Arnold, DO Sub-Investigator: Timothy Wiemkwn, PhD Sub-Investigator: Robert Kelley, PhD Sub-Investigator: James Summersgill, PhD Sub-Investigator: Ruth Carrico, PhD Sub-Investigator: Julie Harting, PharmD Sub-Investigator: Paula Peyrani, MD Principal Investigator: David Seligson, MD Sub-Investigator: Craig Roberts, MD Principal Investigator: Julio Ramirez, MD 收起 << |
| NCT03474198 | Tuberculosis, Pulmonary | Phase 2 Phase 3 | Recruiting | March 12, 2022 | Philippines ... 展开 >> De La Salle Health Sciences Institute Not yet recruiting Manila, Philippines Lung Center Philippines Recruiting Manila, Philippines Philippines Tuberculosis Society Incorporated (PTSI) Not yet recruiting Manila, Philippines Tropical Disease Foundation Not yet recruiting Manila, Philippines Singapore National University Hospital Not yet recruiting Singapore, Singapore Thailand King Chulalongkorn Memorial Hospital Not yet recruiting Bangkok, Thailand 收起 << |
| NCT02689089 | Tuberculosis | Phase 4 | Recruiting | September 2019 | Canada, Ontario ... 展开 >> The Ottawa Hospital - General Campus Recruiting Ottawa, Ontario, Canada, K1H 8L6 Contact: Gonzalo Alvarez, MD 613-737-8899 galvarez@ottawahospital.on.ca Principal Investigator: Gonzalo Alvarez, MD, FRCPC 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.14mL 0.23mL 0.11mL |
5.70mL 1.14mL 0.57mL |
11.40mL 2.28mL 1.14mL |
|
| CAS号 | 61379-65-5 |
| 分子式 | C47H64N4O12 |
| 分子量 | 877.03 |
| SMILES Code | O=C1[C@](C)(OC2=C1C3=C(C(O)=C(NC4=O)C(/C=N/N5CCN(C6CCCC6)CC5)=C3O)C(O)=C2C)O/C=C/[C@@H]([C@H]([C@H]([C@@H]([C@@H]([C@@H]([C@H]([C@H](/C=C/C=C4/C)C)O)C)O)C)OC(C)=O)C)OC |
| MDL No. | MFCD00866806 |
| 别名 | DL 473; Cyclopentylrifampicin; R 773; MDL473 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 50 mg/mL(57.01 mM),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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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