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Other Sizes |
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体外研究 (In Vitro) |
在肌腱细胞中,环丙沙星 (Bay-09867) 盐酸盐一水合物(5–50 μg/mL;0–24 小时)可抑制细胞生长并诱导细胞周期停滞在 G2/M 期[1]。盐酸环丙沙星 (Bay-09867) 一水合物的 MIC90 分别为 0.03 μg/mL 和 0.12 μg/mL,对鼠疫耶尔森菌和炭疽芽孢杆菌表现出强烈的作用[2]。
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体内研究 (In Vivo) |
受到环丙沙星 (Bay-09867) 盐酸盐一水合物的保护(30 mg/kg;腹腔注射;持续 24 小时;BALB/c 小鼠)。小鼠肺鼠疫模型中的鼠疫菌[3]。通过降低主动脉壁中的 LOX 水平并提高 MMP 水平和活性,环丙沙星 (Bay-09867) 盐酸盐一水合物(100 mg/kg;ig;每天,持续 4 周;C57BL/6J 小鼠)加速主动脉根部扩张并提高发病率主动脉夹层和破裂的发生[4]。 Ciprofloxacin (Bay-09867) 盐酸盐一水合物(100 mg/kg;ig;每天,持续 4 周;C57BL/6J 小鼠)会导致线粒体功能障碍、胞质 DNA 传感器信号激活以及 DNA 损伤并释放到胞质中。乳酸环丙沙星可增加主动脉壁的细胞凋亡和坏死性凋亡[4]。
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细胞实验 |
细胞活力测定[1]
细胞类型: 肌腱细胞 测试浓度: 5、10、20 和 50 µg /mL 孵化持续时间:24 小时 实验结果:减少了肌腱细胞的细胞结构。 细胞周期分析[1] 细胞类型: 肌腱细胞 测试浓度: 50 μg/mL 孵育时间:24小时 实验结果:细胞周期被阻滞在G2/M期,并抑制肌腱细胞的细胞分裂。 蛋白质印迹分析[1] 细胞类型: 肌腱细胞 测试浓度: 50 μg/mL 孵育时间:0、6、12、17和24小时 实验结果:下调CDK-1和cyclin B蛋白及mRNA的表达。上调PLK-1蛋白的表达。 |
动物实验 |
Animal/Disease Models: balb/c (Bagg ALBino) mouse[3]
Doses: 30 mg/kg Route of Administration: intraperitoneal (ip)injection; for 24 hrs (hours) Experimental Results: decreased the lung bacterial load in murine model of pneumonic plague. Animal/Disease Models: C57BL/6J mice[4] Doses: 100 mg/kg Route of Administration: po (oral gavage); daily, for 4 weeks Experimental Results: Had aortic destruction that was accompanied by diminished LOX expression and increased MMP expression and activity. Animal/Disease Models: C57BL/ 6J mice[4] Doses: 100 mg/kg Route of Administration: po (oral gavage); daily, for 4 weeks Experimental Results: Caused mitochondrial DNA and nuclear DNA damage, leading to mitochondrial dysfunction and ROS production. Increased apoptosis and necroptosis in the aortic wall. |
毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Amounts of ciprofloxacin in breastmilk are low. Fluoroquinolones such as ciprofloxacin have traditionally not been used in infants because of concern about adverse effects on the infants' developing joints. However, studies indicate little risk. The calcium in milk might decrease absorption of the small amounts of fluoroquinolones in milk, but insufficient data exist to prove or disprove this assertion. Use of ciprofloxacin is acceptable in nursing mothers with monitoring of the infant for possible effects on the gastrointestinal flora, such as diarrhea or candidiasis (thrush, diaper rash). Avoiding breastfeeding for 3 to 4 hours after a dose should decrease the exposure of the infant to ciprofloxacin in breastmilk. Maternal use of an ear drop or eye drop that contains ciprofloxacin presents negligible risk for the nursing infant. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue. ◉ Effects in Breastfed Infants A case of pseudomembranous colitis in a 2-month-old breastfed infant with a history of necrotizing enterocolitis was probably caused by maternal self-treatment with ciprofloxacin. Ciprofloxacin was used as part of multi-drug regimens to treat three pregnant women with multidrug-resistant tuberculosis throughout pregnancy and postpartum. Their three infants were breastfed (extent and duration not stated). At age 1.25, 1.8 and 3.9 years, the children were developing normally except for one who had failure to thrive, possibly due to tuberculosis contracted after birth. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
参考文献 |
[1]. Tsai WC, et, al. Ciprofloxacin-mediated cell proliferation inhibition and G2/M cell cycle arrest in rat tendon cells. Arthritis Rheum. 2008 Jun;58(6):1657-63.
[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 Apr 24;61(5):e02434-16. [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. [4]. LeMaire SA, et, al. Effect of Ciprofloxacin on Susceptibility to Aortic Dissection and Rupture in Mice. JAMA Surg. 2018 Sep 1;153(9):e181804. |
其他信息 |
Ciprofloxacin hydrochloride hydrate is the monohydrate form of ciprofloxacin monohydrochloride. It has a role as an EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor, an antibacterial drug, a topoisomerase IV inhibitor and an antiinfective agent. It contains a ciprofloxacin hydrochloride (anhydrous).
Ciprofloxacin is an antibacterial prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment and prevention of several infections caused by certain types of bacteria, for example, certain urinary tract infections, lower respiratory tract infections, and skin infections. Some bacterial infections can be opportunistic infections (OIs) of HIV. An OI is an infection that occurs more frequently or is more severe in people with weakened immune systems—such as people with HIV—than in people with healthy immune systems. Ciprofloxacin Hydrochloride is the hydrochloride salt form of ciprofloxacin, a fluoroquinolone related to nalidixic acid with antibacterial activity. Ciprofloxacin hydrochloride exerts its bactericidal effect by interfering with the bacterial DNA gyrase, thereby inhibiting the DNA synthesis and preventing bacterial cell growth. A broad-spectrum antimicrobial carboxyfluoroquinoline. See also: Ciprofloxacin (has active moiety); Ciprofloxacin; Ciprofloxacin Hydrochloride (component of); Ciprofloxacin hydrochloride; hydrocortisone (component of) ... View More ... Drug Indication Treatment of chronic pulmonary infections caused by Pseudomonas aeruginosa |
分子式 |
C17H21CLFN3O4MOLECULARWEIGHT
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分子量 |
385.8177
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精确质量 |
385.12
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CAS号 |
86393-32-0
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相关CAS号 |
Ciprofloxacin;85721-33-1;Ciprofloxacin monohydrochloride;93107-08-5;Ciprofloxacin-d8 hydrochloride monohydrate
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PubChem CID |
62998
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外观&性状 |
White to off-white solid powder
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沸点 |
581.8ºC at 760 mmHg
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熔点 |
318-320 °C
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闪点 |
305.6ºC
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LogP |
2.714
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tPSA |
83.8
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氢键供体(HBD)数目 |
4
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氢键受体(HBA)数目 |
8
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可旋转键数目(RBC) |
3
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重原子数目 |
26
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分子复杂度/Complexity |
571
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定义原子立体中心数目 |
0
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SMILES |
Cl.O=C(C1C(=O)C2C(=CC(N3CCNCC3)=C(C=2)F)N(C2CC2)C=1)O.O
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InChi Key |
ARPUHYJMCVWYCZ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C17H18FN3O3.ClH.H2O/c18-13-7-11-14(8-15(13)20-5-3-19-4-6-20)21(10-1-2-10)9-12(16(11)22)17(23)24;;/h7-10,19H,1-6H2,(H,23,24);1H;1H2
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化学名 |
1-cyclopropyl-6-fluoro-4-oxo-7-piperazin-1-ylquinoline-3-carboxylic acid;hydrate;hydrochloride
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意: 请将本产品存放在密封且受保护的环境中,避免吸湿/受潮。 |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
DMSO : ~5 mg/mL (~12.96 mM)
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溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 0.5 mg/mL (1.30 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 5.0 mg/mL澄清DMSO储备液加入400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 0.5 mg/mL (1.30 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 5.0 mg/mL 澄清 DMSO 储备液加入 900 μL 20% SBE-β-CD 生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 0.5 mg/mL (1.30 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5919 mL | 12.9594 mL | 25.9188 mL | |
5 mM | 0.5184 mL | 2.5919 mL | 5.1838 mL | |
10 mM | 0.2592 mL | 1.2959 mL | 2.5919 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。