Ciprofloxacin (Bay-09867) Lactate（5-50 μg/mL；0-24 小时；肌腱细胞）可诱导细胞周期停滞在 G2/M 期并抑制细胞分裂 [1]。乳酸环丙沙星 (Bay-09867) 可有效抑制鼠疫耶尔森氏菌和炭疽杆菌，其 MIC90 分别为 0.03 μg/mL 和 0.12 μg/mL [2]。

在肺鼠疫小鼠模型中，乳酸环丙沙星 (Bay-09867)（30 毫克/千克；腹腔注射；24 小时；BALB/c 小鼠）可预防鼠疫耶尔森菌 [3]。通过降低 LOX 水平并提高 MMP 水平和活性，乳酸环丙沙星 (Bay-09867)（100 毫克/公斤；ig；每日 4 周；C57BL/6J 小鼠）增强并加速主动脉根部增大。主动脉壁破裂和动脉夹层的频率[4]。 Ciprofloxacin (Bay-09867) Lactate（100 mg/kg；IR；每日一次，持续 4 周；C57BL/6J 小鼠）会导致线粒体功能障碍、细胞质 DNA 传感器信号激活以及 DNA 损伤并释放到细胞质中。乳酸环丙沙星会增加主动脉壁的细胞凋亡和坏死性凋亡[4]。

细胞周期分析[1]
细胞类型：肌腱细胞
测试浓度：5、10、20 和 50 μg/mL
孵育持续时间：24小时
实验结果：肌腱细胞的细胞结构减少。

---

细胞凋亡分析 [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，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
孵育持续时间：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。

Animal/Disease Models: balb/c (Bagg ALBino) mouse [3]
Doses: 30 mg/kg
Route of Administration: intraperitoneal (ip) injection; 24-hour
Experimental Results: diminished the bacterial load in the lungs of the plague mouse model.

---

Animal/Disease Models: C57BL/6J mice [4]
Doses: 100 mg/kg
Route of Administration: po (oral gavage); one time/day for 4 weeks
Experimental Results: The aorta was destroyed, accompanied by diminished LOX expression and MMP expression and activity Increase.

---

Animal/Disease Models: C57BL/6J mice [4]
Doses: 100 mg/kg
Route of Administration: po (oral gavage); one time/day for 4 weeks
Experimental Results: Causes mitochondrial DNA and nuclear DNA damage, leading to mitochondrial dysfunction and ROS production. Increased aortic wall cell apoptosis and necroptosis.

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.

[1]. Ciprofloxacin-mediated cell proliferation inhibition and G2/M cell cycle arrest in rat tendon cells. Arthritis Rheum. 2008 Jun;58(6):1657-63.

[2]. 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]. Inhaled Liposomal Ciprofloxacin Protects against a Lethal Infection in a Murine Model of Pneumonic Plague. Front Microbiol. 2017 Feb 6;8:91.

[4]. Effect of Ciprofloxacin on Susceptibility to Aortic Dissection and Rupture in Mice. JAMA Surg. 2018 Sep 1;153(9):e181804.

C20H24FN3O6

421.4195

403.154

97867-33-9

Ciprofloxacin;85721-33-1

149514

Typically exists as solid at room temperature

1.4±0.1 g/cm3

656.4±55.0 °C at 760 mmHg

255-257ºC

350.8±31.5 °C

0.0±2.1 mmHg at 25°C

1.624

0.04

100.87

4

10

4

30

631

0

O=C(C1C(=O)C2C(=CC(N3CCNCC3)=C(C=2)F)N(C2CC2)C=1)O.O=C(C(C)O)O

NRBJWZSFNGZBFQ-UHFFFAOYSA-N

InChI=1S/C17H18FN3O3.C3H6O3/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;1-2(4)3(5)6/h7-10,19H,1-6H2,(H,23,24);2,4H,1H3,(H,5,6)

1-cyclopropyl-6-fluoro-4-oxo-7-piperazin-1-ylquinoline-3-carboxylic acid;2-hydroxypropanoic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

---

注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

View More

注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

---

口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

View More

口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

---

注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

---

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。