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利福喷丁

利福喷丁用途

Rifapentine (Priftin; DL 473)是抗生素,可用于肺结核。

利福喷丁名称

[ CAS 号 ]:
61379-65-5

[ 中文名 ]:
利福喷丁

[ 英文名 ]:
Rifapentine

[中文别名 ]:

[英文别名 ]:

rifamycin-S
Rifamycin-B-tripropyl-hydrazid
Rifapentine
rifamycin-B tripropylhydrazide
EINECS 262-743-9

利福喷丁生物活性

[ 描述 ]:

Rifapentine (Priftin; DL 473)是抗生素,可用于肺结核。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[参考文献]

[1]. Sharma, S.K., 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. 7: p. CD007545.

[相关活性小分子]

利福喷丁物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
969.3±65.0 °C at 760 mmHg

[ 熔点 ]:
179-180ºC

[ 分子式 ]:
C₄₇H₆₄N₄O₁₂

[ 分子量 ]:
877.031

[ 闪点 ]:
540.0±34.3 °C

[ 精确质量 ]:
876.452087

[ PSA ]:
216.66000

[ LogP ]:
2.58

[ 外观性状 ]:
红色-棕色结晶粉末

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.625

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
methanol: soluble2mg/mL, clear, red to red-brown

利福喷丁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: JQ0902000

CHEMICAL NAME :: Rifamycin, 3-(((4-cyclopentyl-1-piperazinyl)imino)methyl)-

CAS REGISTRY NUMBER :: 61379-65-5

LAST UPDATED :: 199712

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C47-H64-N4-O12

MOLECULAR WEIGHT :: 877.15

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 27,242,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 27,242,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3300 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 34,1026,1981

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 710 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 34,1026,1981 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 140 ug/kg/7D-I

TOXIC EFFECTS :: Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.) Biochemical - Metabolism (Intermediary) - other proteins

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 26,720,1991

利福喷丁安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
JQ0902000

[ 海关编码 ]:
2941903000

利福喷丁制备

0.01ml的3-醛基利福霉素SV溶于四氢呋喃，在室温下加入0.011mol的1-氨基-4-环戊基哌嗪。反应用薄层跟踪，至原料点消失，约需麟。蒸去溶剂，剩余物用乙酸乙酯重结晶，得利福喷汀，收率55%，熔点179～180℃。

利福喷丁海关

[ 海关编码 ]: 2941903000

利福喷丁文献

Comparative study of the effects of antituberculosis drugs and antiretroviral drugs on cytochrome P450 3A4 and P-glycoprotein.

Antimicrob. Agents Chemother. 58(6) , 3168-76, (2014)

Predicting drug-drug interactions (DDIs) related to cytochrome P450 (CYP), such as CYP3A4 and one of the major drug transporters, P-glycoprotein (P-gp), is crucial in the development of future chemoth...

Novel Inhaled Combination Powder Containing Amorphous Colistin and Crystalline Rifapentine with Enhanced Antimicrobial Activities against Planktonic Cells and Biofilm of Pseudomonas aeruginosa for Respiratory Infections.

Mol. Pharm. 12 , 2594-603, (2015)

Colistin has been increasingly used for the treatment of respiratory infections caused by Gram-negative bacteria. Unfortunately parenteral administration of colistin can cause severe adverse effects. ...

Bacteriological characterization of a Mycobacterium parascrofulaceum strain isolated from a Chinese pneumonia patient.

Int. J. Infect. Dis. 25 , 82-7, (2014)

A Mycobacterium parascrofulaceum strain was isolated from a pneumonia patient-the first such reported case from China. The bacteriological characteristics of the strain were determined.Species identif...

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