Rifapentine

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Chemical Structure| 61379-65-5 同义名 : DL 473;Cyclopentylrifampicin;R 773;MDL473
CAS号 : 61379-65-5
货号 : A444634
分子式 : C47H64N4O12
纯度 : 98% HPLC
分子量 : 877.031
MDL号 : MFCD00866806
存储条件:

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

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

动物实验配方:
生物活性
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].
临床研究
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 <<
实验方案
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

参考文献

[1]Temple ME, Nahata MC. Rifapentine: its role in the treatment of tuberculosis. Ann Pharmacother. 1999 Nov;33(11):1203-10.

[2]Jarvis B, Lamb HM. Rifapentine. Drugs. 1998 Oct;56(4):607-16; discussion 617.

[3]Sharma SK, Sharma A, Kadhiravan T, Tharyan P. 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

[4]Njie GJ, Morris SB, Woodruff RY, Moro RN, Vernon AA, Borisov AS. Isoniazid-Rifapentine for Latent Tuberculosis Infection: A Systematic Review and Meta-analysis. Am J Prev Med. 2018 Aug;55(2):244-252

[5]Zheng C, Hu X, Zhao L, Hu M, Gao F. Clinical and pharmacological hallmarks of rifapentine's use in diabetes patients with active and latent tuberculosis: do we know enough? Drug Des Devel Ther. 2017 Oct 11;11:2957-2968

[6]Temple ME, Nahata MC. Rifapentine: its role in the treatment of tuberculosis. Ann Pharmacother. 1999 Nov;33(11):1203-10