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利福平

利福平用途

Rifampicin是一种有效的广谱抗生素,可抵抗细菌病原体。

利福平名称

[ CAS 号 ]:
13292-46-1

[ 中文名 ]:
利福平

[ 英文名 ]:
Rifampicin

[中文别名 ]:

[英文别名 ]:

利福平生物活性

[ 描述 ]:

Rifampicin是一种有效的广谱抗生素,可抵抗细菌病原体。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌
研究领域 >> 感染

[体外研究]

利福平(100 mg/mL)可以阻断P-糖蛋白的功能活性。利福平不是P-糖蛋白的减数。利福平耐药的机制与P-糖蛋白的功能活性无关[3]。

[体内研究]

利福平(200,400 mg/kg)可以高浓度诱导脂肪肝[1]。利福平(30 mg/kg,ip)体内处理S464P生物膜导致轻微下降,但与亲本信号相比,这些导管的生物发光早期重新结合,而利福平对感染突变体H481Y的小鼠的生物发光没有影响[2] ]。

[动物实验]

简言之,将携带104cfu金黄色葡萄球菌的1cm Teflon导管(14-gauge)(亲本菌株Xen 29或RifR突变体S464P或H481Y)皮下植入每个菌株9只小鼠的组中。在每只动物的每侧插入一个导管段。植入导管后6天,每组5只小鼠用0.1mg盐水腹膜内30mg / kg的利福平治疗,每天两次,连续4天。每组中剩余的四只小鼠未作为对照处理。在感染期间的不同时间点,使用来自IVIS®歧管的1.5%异氟烷的恒定流量对小鼠进行麻醉,并使用IVIS®ImageSystem 100系列成像。使用LivingImage®软件分析从小鼠发射的生物发光信号(光子/ s)并在感染过程中作图。感染后20天(最终利福平处理后11天)处死小鼠。通过手术移除导管并通过超声处理分离细菌以确定导管上的细菌负荷。

[参考文献]

[1]. Piriou A, et al. Fatty liver induced by high doses of rifampicin in the rat: possible relation with an inhibition of RNA polymerases in eukariotic cells. Arch Toxicol Suppl. 1979;(2):333-7.

[2]. Yu J, et al. Monitoring in vivo fitness of rifampicin-resistant Staphylococcus aureus mutants in a mouse biofilm infection model. J Antimicrob Chemother. 2005 Apr;55(4):528-34. Epub 2005 Mar 2.

[3]. Erokhina MV, et al. [In vitro development of rifampicin resistance in the epithelial cells]. Probl Tuberk Bolezn Legk. 2006;(8):58-61.


[相关活性小分子]

嘌呤霉素二盐酸盐 | G-418 硫酸盐 | 衣霉素 | 潮霉素B | 盐霉素 | 阿维巴坦钠 | 硫酸新霉素 | 法硼巴坦 | 甲氧西林钠 | 甲硝唑 | 羧苄青霉素钠 | 头孢他啶 | 盐酸依拉环素 | 头孢噻肟钠 | 氯霉素

利福平物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
1004.4±65.0 °C at 760 mmHg

[ 熔点 ]:
183ºC (dec.)

[ 分子式 ]:
C43H58N4O12

[ 分子量 ]:
822.940

[ 闪点 ]:
561.3±34.3 °C

[ 精确质量 ]:
822.405151

[ PSA ]:
220.15000

[ LogP ]:
1.09

[ 外观性状 ]:
红色至橙色结晶固体

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.613

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
chloroform: soluble50mg/mL, clear

利福平MSDS

利福平毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VJ7000000
CHEMICAL NAME :
Rifomycin SV, 8-(N-(4-methyl-1-piperazinyl)formidoyl)-
CAS REGISTRY NUMBER :
13292-46-1
LAST UPDATED :
199607
DATA ITEMS CITED :
60
MOLECULAR FORMULA :
C43-H58-N4-O12
MOLECULAR WEIGHT :
823.05
WISWESSER LINE NOTATION :
T C6 B65-24- A D E 2BC G& AV LO NO F&VM OU B&U D&U MH&&&TJ DQ GQ IQ JI MI QO1 R1 SOV1 T1 UQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
504 mg/kg/42D-I
TOXIC EFFECTS :
Behavioral - muscle weakness Lungs, Thorax, or Respiration - dyspnea Blood - aplastic anemia
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
315 mg/kg/5W-I
TOXIC EFFECTS :
Skin and Appendages - dermatitis, other (after systemic exposure)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
180 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - conjunctive irritation Sense Organs and Special Senses (Eye) - iritis Skin and Appendages - dermatitis, other (after systemic exposure)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
13 mg/kg/2D
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - effect, not otherwise specified
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
857 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Gastrointestinal - other changes Skin and Appendages - dermatitis, other (after systemic exposure)
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1570 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
511 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
534 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
416 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
621 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
260 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
2120 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
639 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
4 gm/kg/8D-I
TOXIC EFFECTS :
Liver - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
17500 mg/kg/5W-I
TOXIC EFFECTS :
Liver - fatty liver degeneration Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
72800 mg/kg/26W-I
TOXIC EFFECTS :
Liver - other changes Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Related to Chronic Data - death
TYPE OF TEST :
TCLo - Lowest published toxic concentration
ROUTE OF EXPOSURE :
Inhalation
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
5 mg/m3/4H/17W-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Lungs, Thorax, or Respiration - fibrosis, focal (pneumoconiosis) Lungs, Thorax, or Respiration - changes in lung weight
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
280 mg/kg/14D-I
TOXIC EFFECTS :
Liver - change in gall bladder structure or function Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
7800 mg/kg/26W-I
TOXIC EFFECTS :
Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
19005 mg/kg/26W-I
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
11200 mg/kg/4W-I
TOXIC EFFECTS :
Liver - jaundice, other or unclassified Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
5600 mg/kg/8D-I
TOXIC EFFECTS :
Liver - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death
TYPE OF TEST :
TCLo - Lowest published toxic concentration
ROUTE OF EXPOSURE :
Inhalation
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
5 mg/m3/4H/17W-I
TOXIC EFFECTS :
Cardiac - changes in heart weight Lungs, Thorax, or Respiration - fibrosis, focal (pneumoconiosis) Lungs, Thorax, or Respiration - changes in lung weight
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
8400 mg/kg/60W-C
TOXIC EFFECTS :
Tumorigenic - neoplastic by RTECS criteria Liver - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1400 mg/kg
SEX/DURATION :
female 4-10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
3200 mg/kg
SEX/DURATION :
female 1-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
4 gm/kg
SEX/DURATION :
female 2-21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
800 mg/kg
SEX/DURATION :
female 9-12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - urogenital system
TYPE OF TEST :
TCLo - Lowest published toxic concentration
ROUTE OF EXPOSURE :
Inhalation
DOSE :
6100 ug/m3/24H
SEX/DURATION :
female 1-22 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - physical
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2200 mg/kg
SEX/DURATION :
female 6-16 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2600 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

MUTATION DATA

TYPE OF TEST :
Host-mediated assay
TEST SYSTEM :
Rodent - mouse Ascites tumor
DOSE/DURATION :
5 mg/kg
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 141,171,1984 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 24,243,1980 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 24,243,1980 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987 TOXICOLOGY REVIEW MMWOAU Muenchener Medicinische Wochenschrift. (Munich, Fed. Rep. Ger.) V.33-115, 1886-1973. Volume(issue)/page/year: 115,1685,1973 TOXICOLOGY REVIEW LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 2,1285,1980 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4882 No. of Facilities: 141 (estimated) No. of Industries: 1 No. of Occupations: 3 No. of Employees: 928 (estimated) No. of Female Employees: 656 (estimated)

利福平安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
VJ7000000

[ 海关编码 ]:
2941903000

利福平合成路线

利福平上下游产品

利福平制备

利福平是利福霉素SV的半合成衍生物。将利福霉素SV氧化成利福霉素S,再与甲醛、叔丁胺进行甲酰化反应生成3-甲酰基叔丁胺利福霉素S,然后用维生素C还原、与1-甲基-4-氨基哌嗪缩合而得利福平。

利福平海关

[ 海关编码 ]: 2941903000

利福平文献

Enhancement of in vitro activity of tuberculosis drugs by addition of thioridazine is not reflected by improved in vivo therapeutic efficacy.

Tuberculosis (Edinb.) 94(6) , 701-7, (2015)

Assessment of the activity of thioridazine towards Mycobacterium tuberculosis (Mtb), in vitro and in vivo as a single drug and in combination with tuberculosis (TB) drugs.The in vitro activity of thio...

Disruption of an M. tuberculosis membrane protein causes a magnesium-dependent cell division defect and failure to persist in mice.

PLoS Pathog. 11(2) , e1004645, (2015)

The identification of Mycobacterium tuberculosis genes necessary for persistence in vivo provides insight into bacterial biology as well as host defense strategies. We show that disruption of M. tuber...

Kinetics of recA and recX induction in drug-susceptible and MDR clinical strains of Mycobacterium tuberculosis.

J. Antimicrob. Chemother. 69(12) , 3199-202, (2014)

To investigate and compare the expression of recA and recX, components of the SOS pathway, following rifampicin treatment in drug-susceptible and MDR clinical strains of Mycobacterium tuberculosis.Str...


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产品详情:[Perfemiker]利福平,98%生物技术级


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标题:利福平_MSDS_用途_密度_利福平CAS号【13292-46-1】_化源网 地址:https://www.chemsrc.com/amp/cas/13292-46-1_832351.html