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Merck
CN

R0533

利福喷丁

别名:

3-(((4-cyclopentyl-1-piperazinyl)imino)methyl)rifamycin, Cyclopentylrifampicin, DL 473

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关于此项目

经验公式（希尔记法）:
C47H64N4O12
化学文摘社编号:
61379-65-5
分子量:
877.03
EC 号:
262-743-9
UNSPSC代码:
51283603
PubChem化学物质编号:
329823987
NACRES:
NA.85

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方案

≥93.5%

质量水平

200

表单

powder or crystals

抗生素抗菌谱

Gram-negative bacteria
Gram-positive bacteria
mycobacteria

作用机制

enzyme | inhibits

储存温度

2-8°C

SMILES字符串

N5(CCN(CC5)C6CCCC6)N=Cc1c2c(c3c(c4c(c(c3O)C)O[C@](O\C=C\C([C@H]([C@H]([C@@H]([C@@H]([C@@H]([C@H]([C@H](\C=C\C=C(/C(=O)N2)\C)C)O)C)O)C)OC(=O)C)C)OC)(C4=O)C)c1O)O

InChI

1S/C47H64N4O12/c1-24-13-12-14-25(2)46(59)49-37-32(23-48-51-20-18-50(19-21-51)31-15-10-11-16-31)41(56)34-35(42(37)57)40(55)29(6)44-36(34)45(58)47(8,63-44)61-22-17-33(60-9)26(3)43(62-30(7)52)28(5)39(54)27(4)38(24)53/h12-14,17,22-24,26-28,31,33,38-39,43,53-57H,10-11,15-16,18-21H2,1-9H3,(H,49,59)/b13-12+,22-17+,25-14-,48-23?/t24-,26+,27+,28+,33?,38-,39+,43+,47-/m0/s1

InChI key

WDZCUPBHRAEYDL-OABFQHKQSA-N

相关类别

一般描述

Chemical structure: macrolide

应用

Rifapentine is an antibiotic clinically used to treat tuberculosis. It is used in tuberculosis research.

生化/生理作用

Rifapentine is a semisynthetic derivative of rifampicin with antibacterial activity against Gram-positive and Gram-negative bacteria and against Mycobacterium tuberculosis. Rifapentine inhibits DNA-dependant RNA polymerase and prevents RNA transcription. It interacts with bacterial RNA polymerase but does not inhibit the mammalian enzyme.
Semisynthetic derivative of rifampicin with antibacterial activity against Gram-positive and Gram-negative bacterial and against Mycobacterium tuberculosis. Rifapentine inhibits DNA-dependant RNA polymerase and prevents RNA transcription.

其他说明

Keep container tightly closed in a dry and well-ventilated place.

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H315,H319,H335

预防措施声明

P261 - P305 + P351 + P338

危险分类

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

涉药品监管产品
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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000474742
0000474742
0000398815
0000398816
0000377954

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Kelly E Dooley et al.
The lancet. HIV, 7(6), e401-e409 (2020-04-03)
Short-course preventive therapy with 12 doses of once-weekly rifapentine (900 mg) plus isoniazid (900 mg) could greatly improve tuberculosis control, especially in areas with high co-endemicity with HIV. However, a small previous trial of such therapy with dolutegravir in healthy
Simbarashe P Zvada et al.
Antimicrobial agents and chemotherapy, 56(8), 4471-4473 (2012-05-16)
We described the population pharmacokinetics of moxifloxacin and the effect of high-dose intermittent rifapentine in patients with pulmonary tuberculosis who were randomized to a continuation-phase regimen of 400 mg moxifloxacin and 900 mg rifapentine twice weekly or 400 mg moxifloxacin
Ruth N Moro et al.
Annals of the American Thoracic Society, 15(5), 570-580 (2018-02-03)
Data are limited regarding the safety of 12-dose once-weekly isoniazid (H, 900 mg) plus rifapentine (P, 900 mg) (3HP) for latent infection treatment during pregnancy. To assess safety and pregnancy outcomes among pregnant women who were inadvertently exposed to study
Kathy Williams et al.
Antimicrobial agents and chemotherapy, 56(6), 3114-3120 (2012-04-04)
Novel oral regimens composed of new drugs with potent activity against Mycobacterium tuberculosis and no cross-resistance with existing agents are needed to shorten and simplify treatment for both drug-susceptible and drug-resistant tuberculosis. As part of a continuing effort to evaluate
Susan E Dorman et al.
The Journal of infectious diseases, 206(7), 1030-1040 (2012-08-02)
Rifapentine administered 5 days per week has potent activity in mouse models of antituberculosis chemotherapy, but efficacy and safety data are limited in humans. We compared the antimicrobial activity and safety of rifapentine vs rifampin during the first 8 weeks
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