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环丙沙星

环丙沙星用途

Ciprofloxacin 是一种氟喹诺酮类抗生素,具有高效的抗菌 (antibacterial) 活性。

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环丙沙星名称

[ CAS 号 ]:
85721-33-1

[ 中文名 ]:
环丙沙星

[ 英文名 ]:
Ciprofloxacin

[中文别名 ]:

[英文别名 ]:

CPFX
ciproiv
CIPROBAY
euciprin
Cipro
Ciprine
ciloxan
Ciprofloxacin
Cipmbay
ciprobid

环丙沙星生物活性

[ 描述 ]:

Ciprofloxacin 是一种氟喹诺酮类抗生素,具有高效的抗菌 (antibacterial) 活性。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[体外研究]

环丙沙星是一种氟喹诺酮类抗生素,具有很强的抗菌活性[1]。环丙沙星(CIP)显示出对抗鼠疫菌的强效活性,MIC90为0.03μg/ mL [2]。

[体内研究]

与暴露于恩诺沙星的幼虫的抑制GST和过氧化氢酶(CAT)相比,环丙沙星(1mg/L)诱导谷胱甘肽-S-转移酶(GST)活性。环丙沙星(≥10μg/ L)和恩诺沙星对anuran两栖类幼虫的发育,生长,解毒和氧化应激酶具有生态毒性[1]。在肺鼠疫的小鼠模型中,环丙沙星(30mg/kg,ip)导致药物暴露,其类似于在500mg剂量的口服环丙沙星后在人中观察到的药物暴露。与腹膜内PBS治疗对照相比,腹腔内环丙沙星可降低肺部细菌负荷[3]。

[细胞实验]

通过将菌落悬浮于Mueller-Hinton肉汤（CAMHB）（含有环丙沙星）18至24小时（炭疽芽孢杆菌）或42至48小时（鼠疫杆菌）的绵羊血琼脂（SBA）平板上制备细菌接种物。在35°C。用CAMHB将悬浮的培养物稀释至基于600nm处的光密度调节的105CFU / mL的细菌细胞密度。向96孔板的每个孔中加入50μL稀释液，用于~5×10 4 CFU /孔的最终接种物。将板在35℃温育。在18至24小时（炭疽芽孢杆菌）或42至48小时（鼠疫杆菌）以及600纳米的吸光度下目测确定MIC [2]。

[动物实验]

在该测定中使用8至10周龄的雌性BALB / cAnNCr1（BALB / c）小鼠和20g（±4g）。通过腹膜内（ip）途径向小鼠（n = 30）施用单剂量的环丙沙星（30mg / kg）。小鼠（n = 3 /时间点/组）在环丙沙星给药后1小时，10分钟，20分钟或30分钟和1,1.5,2,4,8,12小时和1,15或30分钟和1小时剔除DRCFI或CFI施用后2小时，4小时，6小时，10小时，18小时或24小时。根据环丙沙星的短半衰期和较长的CFI半衰期选择血液采样点。在死后收集血液和肺（整个器官）用于分析。给予CFI或DRCFI后的肺剂量使用给药后1分钟肺样品中环丙沙星的浓度计算[3]。

[参考文献]

[1]. Peltzer PM, et al. Ecotoxicity of veterinary enrofloxacin and ciprofloxacin antibiotics on anuran amphibian larvae. Environ Toxicol Pharmacol. 2017 Feb 4. pii: S1382-6689(17)30029-7

[2]. Steenbergen J, et al. In Vitro and In Vivo Activity of Omadacycline Against Two Biothreat Pathogens: Bacillus anthracis and Yersinia pestis. Antimicrob Agents Chemother. 2017 Feb 21.

[3]. Hamblin KA, et al. Inhaled Liposomal Ciprofloxacin Protects against a Lethal Infection in a Murine Model of Pneumonic Plague. Front Microbiol. 2017 Feb 6;8:91.

[相关活性小分子]

环丙沙星物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
581.8±50.0 °C at 760 mmHg

[ 熔点 ]:
255-257°C

[ 分子式 ]:
C₁₇H₁₈FN₃O₃

[ 分子量 ]:
331.341

[ 闪点 ]:
305.6±30.1 °C

[ 精确质量 ]:
331.133209

[ PSA ]:
74.57000

[ LogP ]:
0.65

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.655

[ 储存条件 ]:
Store at 0-5°C

[ 水溶解性 ]:
水溶性：不溶；不溶：乙醇

环丙沙星MSDS

详细MSDS(安全技术说明书)

环丙沙星毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VB1993800

CHEMICAL NAME :: 3-Quinolinecarboxylic acid, 1,4-dihydro-1-cyclopropyl-6-fluoro-4-oxo-7-(1-piperaz inyl)-

CAS REGISTRY NUMBER :: 85721-33-1

LAST UPDATED :: 199709

DATA ITEMS CITED :: 29

MOLECULAR FORMULA :: C17-H18-F-N3-O3

MOLECULAR WEIGHT :: 331.38

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 21429 ug/kg/3D-I

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 21 mg/kg/3D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - urine volume decreased Kidney, Ureter, Bladder - proteinuria Kidney, Ureter, Bladder - hematuria

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 5714 ug/kg/2D-I

TOXIC EFFECTS :: Behavioral - coma Liver - jaundice, other or unclassified Liver - liver function tests impaired

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 129 mg/kg/6D-I

TOXIC EFFECTS :: Behavioral - rigidity (including catalepsy)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 135 mg/kg/3D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 40 mg/kg/2D-I

TOXIC EFFECTS :: Behavioral - headache Blood - eosinophilia Nutritional and Gross Metabolic - body temperature increase

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Multiple routes

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 40 mg/kg/6D-I

TOXIC EFFECTS :: Skin and Appendages - dermatitis, allergic (after systemic exposure) 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 :: >2 gm/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 :: >1 gm/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 - rat

DOSE/DURATION :: 207 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5 gm/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 :: 1165 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 :: >1 gm/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 :: 122 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity)

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Sister chromatid exchange

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Mammal - domestic Cells - not otherwise specified

DOSE/DURATION :: 27 mg/L

REFERENCE :: AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 34,1955,1990

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环丙沙星安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ WGK德国 ]:
2

[ RTECS号 ]:
VB1993800

[ 海关编码 ]:
3004909090

环丙沙星合成路线

详细合成路线

环丙沙星上下游产品

环丙沙星上游产品

环丙沙星下游产品

环丙沙星制备

1.其合成是从2,4-二氯甲苯开始，经硝化、还原、氟化、氯化、水解和酰氯化形成2,4-二氯-5氟苯甲酰氯。然后先后和丙酸二乙酯，对甲苯磺酸，原甲酸三乙酯，环丙胺反应后再环合得喹啉环。经水解，再引入哌嗪基，最后得产品。

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环丙沙星海关

[ 海关编码 ]: 3004909090

环丙沙星文献

A short splice form of Xin-actin binding repeat containing 2 (XIRP2) lacking the Xin repeats is required for maintenance of stereocilia morphology and hearing function.

J. Neurosci. 35(5) , 1999-2014, (2015)

Approximately one-third of known deafness genes encode proteins located in the hair bundle, the sensory hair cell's mechanoreceptive organelle. In previous studies, we used mass spectrometry to charac...

NADPH oxidase expression and production of superoxide by human corneal stromal cells.

Mol. Vis. 15 , 2535-43, (2009)

Superoxide (O(2) (.-)) may function as a second messenger or regulator of signal transduction when produced at low concentrations in the proper locations within cells. The purpose of these studies was...

Genotypes and oxacillin resistance of Staphylococcus aureus from chicken and chicken meat in Poland.

Poult. Sci. 93(12) , 3179-86, (2014)

The genotypes and oxacillin resistance of 263 Staphylococcus aureus isolates cultured from chicken cloacae (n = 138) and chicken meat (n = 125) was analyzed. Fifteen spa types were determined in the s...

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环丙沙星

环丙沙星用途

环丙沙星名称

环丙沙星生物活性

环丙沙星物理化学性质

环丙沙星MSDS

详细MSDS(安全技术说明书)

环丙沙星毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

环丙沙星安全信息

环丙沙星合成路线

详细合成路线

环丙沙星上下游产品

环丙沙星上游产品

环丙沙星下游产品

环丙沙星制备

环丙沙星海关

环丙沙星文献

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