Ciprofloxacin HCl hydrate (Bay-09867)

别名: 盐酸环丙沙星;盐酸环丙沙星(一水物);1-环丙基-6-氟-1,4-二氢-4-氧代-7-(1-哌嗪基)-3-喹啉羧酸盐酸盐一水物;环丙沙星盐酸盐一水合物;盐酸环丙沙星一水物; 盐酸环丙沙星(一水物)标准品; 环丙沙星;环丙沙星(盐酸盐) 标准品;环丙沙星盐酸;环丙沙星盐酸盐;乳酸环丙沙星; 盐酸环丙沙星 EP标准品;盐酸环丙沙星 USP标准品;盐酸环丙沙星(兽用);盐酸环丙沙星标准品;盐酸环丙沙星峰鉴别 EP标准品;盐酸环丙沙星一水合物标准品;
目录号: V13232 纯度: ≥98%
盐酸环丙沙星水合物(也称为 Bay-09867)是一种广谱羧基氟喹诺酮抗生素/抗菌剂,可干扰细菌 DNA 旋转酶,抑制 DNA 合成,并防止细菌细胞生长。
Ciprofloxacin HCl hydrate (Bay-09867) CAS号: 86393-32-0
产品类别: Antibiotics
产品仅用于科学研究,不针对患者销售
规格 价格 库存 数量
1g
2g
5g
10g
25g
50g
100g
Other Sizes

Other Forms of Ciprofloxacin HCl hydrate (Bay-09867):

  • Desethylene Ciprofloxacin-d4 hydrochloride
  • Ciprofloxacin-d8 hydrochloride hydrate (Bay-09867-dd8 (hydrochloride hydrate))
  • Ciprofloxacin-d8 hydrochloride monohydrate (Bay-09867-d8 (hydrochloride monohydrate))
  • Ciprofloxacin-13C3,15N monohydrochloride
  • N-Acetylciprofloxacin
  • 环丙沙星
  • 环丙沙星盐酸盐
点击了解更多
InvivoChem产品被CNS等顶刊论文引用
纯度/质量控制文件

纯度: ≥98%

产品描述
盐酸环丙沙星水合物(也称为 Bay-09867)是一种广谱羧基氟喹诺酮抗生素/抗菌剂,干扰细菌 DNA 旋转酶,抑制 DNA 合成,并防止细菌细胞生长。对于肠杆菌科、铜绿假单胞菌、流感嗜血杆菌、淋病奈瑟菌、链球菌、金黄色葡萄球菌和脆弱拟杆菌菌株,其 MIC90(90% 的最低抑制浓度)在 0.008 至 2 μg/ml 之间。环丙沙星抑制拓扑异构酶 IV 作为主要拓扑异构酶靶标,抑制促旋酶作为次要靶标。
生物活性&实验参考方法
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]。
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]。
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
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C17H21CLFN3O4MOLECULARWEIGHT
分子量
385.8177
精确质量
385.12
CAS号
86393-32-0
相关CAS号
Ciprofloxacin;85721-33-1;Ciprofloxacin monohydrochloride;93107-08-5;Ciprofloxacin-d8 hydrochloride monohydrate
PubChem CID
62998
外观&性状
White to off-white solid powder
沸点
581.8ºC at 760 mmHg
熔点
318-320 °C
闪点
305.6ºC
LogP
2.714
tPSA
83.8
氢键供体(HBD)数目
4
氢键受体(HBA)数目
8
可旋转键数目(RBC)
3
重原子数目
26
分子复杂度/Complexity
571
定义原子立体中心数目
0
SMILES
Cl.O=C(C1C(=O)C2C(=CC(N3CCNCC3)=C(C=2)F)N(C2CC2)C=1)O.O
InChi Key
ARPUHYJMCVWYCZ-UHFFFAOYSA-N
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
化学名
1-cyclopropyl-6-fluoro-4-oxo-7-piperazin-1-ylquinoline-3-carboxylic acid;hydrate;hydrochloride
HS Tariff Code
2934.99.9001
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)
溶解度数据
溶解度 (体外实验)
DMSO : ~5 mg/mL (~12.96 mM)
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。

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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。
例如,若需制备1 mL的工作液,可将 100 μL 5.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。


请根据您的实验动物和给药方式选择适当的溶解配方/方案:
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。

计算器

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度,具体如下:

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示:
假如化合物的分子量为350.26 g/mol,在5mL DMSO中制备10mM储备液所需的化合物的质量是多少?
  • 在分子量(MW)框中输入350.26
  • 在“浓度”框中输入10,然后选择正确的单位(mM)
  • 在“体积”框中输入5,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式,您可以计算体积和浓度。

稀释计算器可计算如何稀释已知浓度的储备液。例如,可以输入C1、C2和V2来计算V1,具体如下:

制备25毫升25μM溶液需要多少体积的10 mM储备溶液?
使用方程式C1V1=C2V2,其中C1=10mM,C2=25μM,V2=25 ml,V1未知:
  • 在C1框中输入10,然后选择正确的单位(mM)
  • 在C2框中输入25,然后选择正确的单位(μM)
  • 在V2框中输入25,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案62.5μL(0.1 ml)出现在V1框中
g/mol

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成,具体如下:

注:化学分子式大小写敏感:C12H18N3O4  c12h18n3o4
计算化合物摩尔质量(分子量)的说明:
  • 要计算化合物的分子量 (摩尔质量),请输入化学/分子式,然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义:
  • 分子质量(或分子量)是一种物质的一个分子的质量,用统一的原子质量单位(u)表示。(1u等于碳-12中一个原子质量的1/12)
  • 摩尔质量(摩尔重量)是一摩尔物质的质量,以g/mol表示。
/

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器(澄清溶液)
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶/难溶于水的化合物),不同的产品和批次配方组成不同,如对配方有疑问,可先联系我们提供正确的体内实验配方。此外,请注意这只是一个配方计算器,而不是特定产品的确切配方。
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+
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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) 。

生物数据图片
  • Study 1. Shown is the survival of mice infected with B. anthracis Ames following treatment with omadacycline, doxycycline, or ciprofloxacin (all given i.p.). n = 10 for all groups.[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.
  • Study 2, postexposure prophylaxis. Shown is the survival of mice infected with B. anthracis Ames following treatment with omadacycline, doxycycline, or ciprofloxacin (all given i.p.). n = 10 for all groups (n = 9 for ciprofloxacin). The MIC for ciprofloxacin and doxycycline was 0.03 μg/ml, and for omadacycline it was ≤0.03 μg/ml.[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.
  • Study 2, delayed treatment (48 h after treatment initiation). Shown is the survival of mice infected with B. anthracis Ames following treatment with omadacycline, doxycycline, or ciprofloxacin (all given i.p.). n = 10 for all groups (n = 9 for ciprofloxacin). The MIC for ciprofloxacin and doxycycline was 0.03 μg/ml, and for omadacycline it was ≤0.03 μg/ml.[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.
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