105956-97-6|Clinafloxacin hydrochloride|Clinafloxacin hydrochloride, fluoroquinolone antibiotic|MFCD00865120-范德生物科技公司

Clinafloxacin hydrochloride

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names：
Clinafloxacin hydrochloride, fluoroquinolone antibiotic
CAS号：
105956-97-6
MDL Number： MFCD00865120
MF(分子式)： C17H17ClFN3O3 MW(分子量)： 365.79
EINECS: Reaxys Number:
Pubchem ID:60063 Brand:BIOFOUNT

克林沙星(105956-97-6,Clinafloxacin,PD-127391)是一种氟喹诺酮类抗生素，克林沙星具有广泛的抗菌活性。克林沙星同时抑制DNA促旋酶和拓扑异构酶IV。

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中文别名	Clinafloxacin hydrochloride(105956-97-6);克林沙星;7-（3-氨基-1-吡咯烷基）-8-氯-1-环丙基-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸;7-（3-氨基吡咯烷-1-基）-8-氯-1-环丙基-6-氟-4-氧代-1,4-二氢喹啉-3-羧酸；
英文别名	Clinafloxacin hydrochloride, fluoroquinolone antibiotic(105956-97-6);AM 1091;AM-1091;CI 960;CI-960;clinafloxacin;PD 127,391;PD 127391;PD-127,391;PD-127391;PD127,391;;7-(3-amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid; 7-(3-aminopyrrolidin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid;
CAS号	105956-97-6
Inchi	InChI=1S/C17H17ClFN3O3/c18-13-14-10(5-12(19)15(13)21-4-3-8(20)6-21)16(23)11(17(24)25)7-22(14)9-1-2-9/h5,7-9H,1-4,6,20H2,(H,24,25)CopyCopied
InchiKey	QGPKADBNRMWEQR-UHFFFAOYSA-NCopyCopied
分子式 Formula	C17H17ClFN3O3
分子量 Molecular Weight	365.79
溶解度Solubility	生物体外In Vitro:DMSO溶解度2 mg/mL(5.47 mM;ultrasonic and warming and heat to 80°C)
性状	浅米色固体
储藏条件 Storage conditions	-20°C Freezer

克林沙星(105956-97-6,Clinafloxacin,PD-127391)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
152. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:克林沙星试剂,克林沙星杂质,克林沙星合成,克林沙星密度,克林沙星溶解度,克林沙星中间体,克林沙星闪点,克林沙星熔点,克林沙星结构式,克林沙星购买,

产品说明	克林沙星(105956-97-6,Clinafloxacin,PD-127391)可以作为药物杂质对照品以及生物医药类试剂。
Introduction	克林沙星(105956-97-6,Clinafloxacin,PD-127391)can be used as a reference substance for drug impurities and reagents，only for research.
Application1
Application2
Application3

克林沙星(105956-97-6,Clinafloxacin,PD-127391)药理学：

1、克林沙星是目前正在研究的氟喹诺酮类抗菌剂。已证明具有良好的抗生素特性。但是，由于存在严重的副作用，其批准和发布已被暂停。7-（3-氨基-1-吡咯烷基）-8-氯-1-环丙基-6-氟-4-氧代-3-喹啉羧酸是喹啉的成员。

2、克林沙星是拓扑异构酶II抑制剂，克林沙星可以抑制DNA拓扑异构酶II活性的化合物。包括在该类别中的是靶向拓扑异构酶II的真核形式的多种抗肿瘤剂和靶向于拓扑异构酶II的原核形式的抗微生物剂。

3、克林沙星是抗菌剂，克林沙星可以抑制细菌生长或繁殖的物质。

4、克林沙星（PD-127391）是氟喹诺酮类抗生素。目标：抗菌药物克林沙星是一种广谱抗生素，目前正在开发用于严重感染的静脉内和口服治疗的喹诺酮羧酸类。Clinafloxacin是一种新型的氟喹诺酮，对革兰氏阳性，革兰氏阴性和厌氧菌具有强大的广谱体外活性。Clinafloxacin对肺炎链球菌7785具有很高的活性（MIC，0.125μg/ mL），单独的gyrA和parC喹诺酮耐药性突变都对这种活性没有太大影响。与氧氟沙星，左氧氟沙星，司巴沙星，格帕沙星相比，克林沙星被认为是对肺炎链球菌最具活性的氟喹诺酮。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H333吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P313获得医疗建议/护理
备注	Clinafloxacin实验过程中防止吸入、食入，做好安全防护

克林沙星(105956-97-6,Clinafloxacin,PD-127391)危害标识：

象形图
信号	Warning
GHS危险说明	Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory.
	H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]
	Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范说明代码	P201, P202, P281, P308+P313, P405, and P501
防范说明代码	(The corresponding statement to each P-code can be found at the GHS Classification page.)

Humphrey, G.H., et al., Pharmacokinetics of clinafloxacin enantiomers in humans. J Clin Pharmacol, 1999. 39(11): p. 1143-50.

Pan, X.S. and L.M. Fisher, DNA gyrase and topoisomerase IV are dual targets of clinafloxacin action in Streptococcus pneumoniae. Antimicrob Agents Chemother, 1998. 42(11): p. 2810-6.

Jorgensen, J.H., et al., Activities of clinafloxacin, gatifloxacin, gemifloxacin, and trovafloxacin against recent clinical isolates of levofloxacin-resistant Streptococcus pneumoniae. Antimicrob Agen

Ciprofloxacin and Clinafloxacin Antibodies for an Immunoassay of Quinolones: Quantitative Structure?Activity Analysis of Cross-Reactivities PMID 30641870; International journal of molecular sciences 2

In vitro activities of 11 fluoroquinolones against 226 Campylobacter jejuni strains isolated from Finnish patients, with special reference to ciprofloxacin resistance PMID 16223936; The Journal of ant

克林沙星(105956-97-6,Clinafloxacin,PD-127391)参考文献：

1.Synthesis of (99m)TcN-clinafloxacin Dithiocarbamate Complex and Comparative Radiobiological Evaluation in Staphylococcus aureus Infected Mice.
Shah SQ1, Khan MR2. World J Nucl Med. 2014 Sep;13(3):154-8. doi: 10.4103/1450-1147.144813.

Clinafloxacin dithiocarbamate (CNND) preparation and radiolabeling through [(99m)Tc ≡ N](2+) core with the gamma (γ) emitter ((99m)Tc) was assessed. The potentiality of the (99m)Tc(V) ≡ N-CNND complex was investigated as perspective a Staphylococcus aureus (S.a.) in vivo infection radiotracer in terms of radiochemical stability in normal saline (n.s.), human serum (h.s.), binding efficacy with live and heat killed S.a. and biodistribution in female nude mice model (FNMD). More than 90% stability was observed in n.s. for 4 h with the highest yield of 98.70 ± 0.26% at 30 min after reconstitution. In h.s., the (99m)Tc(V) ≡ N-CNND complex was found stable up to 16 h with 15.35% side products. Maximum in vitro binding (68.75 ± 0.80%, 90 min) with S.a. was observed after 90 min of incubation. In FNMD, (infected with live strain) approximately six-fold higher uptakes was noted in the infected to inflamed and normal muscles. The higher stability in n.

2.Design and biological evaluation of novel quinolone-based metronidazole derivatives as potent Cu(2+) mediated DNA-targeting antibacterial agents.
Zhang L1, Kumar KV1, Geng RX2, Zhou CH3. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3699-705. doi: 10.1016/j.bmcl.2015.06.041. Epub 2015 Jun 16.

A series of novel quinolone-based metronidazole derivatives as new type of antimicrobial agents were developed and characterized. Most of them gave good antibacterial activity towards the Gram-positive and negative bacteria. Noticeably, quinolone derivative 3i exhibited low MIC value of 0.25 μg/mL against Pseudomonas aeruginosa, which was even superior to reference drugs Norfloxacin, Ciprofloxacin and Clinafloxacin. The further research revealed that compound 3i could intercalate into P. aeruginosa DNA through copper ion bridge to form a steady 3i-Cu(2+)-DNA ternary complex which might further block DNA replication to exert the powerful bioactivities.

3.Heat stable antimicrobial activity of Burkholderia gladioli OR1 against clinical drug resistant isolates.
Bharti P1, Anand V, Chander J, Singh IP, Singh TV, Tewari R. Indian J Med Res. 2012 May;135(5):666-71.

BACKGROUND & OBJECTIVES: Drug resistant microbes are a serious challenge to human health. During the search for novel antibiotics/inhibitors from the agricultural soil, a bacterial colony was found to inhibit the growth of clinical isolates including Staphylococcus (resistant to amikacin, ciprofloxacin, clindamycin, clinafloxacin, erythromycin, gentamicin and methicillin) and Candida (resistant to fluconazole and itraconazole). The culture was identified as Burkholderia gladioli and produced at least five different antimicrobial compounds which were highly stable at high temperature (121 o C) and in the broad pH range (3.0-11.0). We report here the antimicrobial activity of B. gladioli against drug resistant bacterial pathogens.

4.Relationship of cellular topoisomerase IIα inhibition to cytotoxicity and published genotoxicity of fluoroquinolone antibiotics in V79 cells.
Williams GM1, Brunnemann KD, Smart DJ, Molina D, Jeffrey AM, Duan JD, Krebsfaenger N, Kampkoetter A, Schmuck G. Chem Biol Interact. 2013 Apr 25;203(2):386-90. doi: 10.1016/j.cbi.2013.01.003. Epub 2013 Jan 20.

Fluoroquinolone (FQ) antibiotics are bacteriocidal through inhibition of the bacterial gyrase and at sufficient concentrations in vitro, they can inhibit the homologous eukaryotic topoisomerase (TOPO) II enzyme. FQ exert a variety of genotoxic effects in mammalian systems through mechanisms not yet established, but which are postulated to involve inhibition of TOPO II enzymes. To assess the relationship of inhibition of cell nuclear TOPO II to cytotoxicity and reported genotoxicity, two FQ, clinafloxacin (CLFX) and lomefloxacin (LOFX), having available genotoxicity data showing substantial differences with CLFX being more potent than LOFX, were selected for study. The relative inhibitory activities of these FQ on nuclear TOPO IIα in cultured Chinese hamster lung fibroblasts (V79 cells) over dose ranges and at equimolar concentrations were assessed by measuring nuclear stabilized cleavage complexes of TOPO IIα-DNA. Cytotoxicity was measured by relative cell counts.

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