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100mg | ||
250mg | ||
500mg |
ln Vitro |
Ciprofloxacin (Bay-09867) Lactate (5-50 μg/mL; 0-24 hours; tenocytes) induces cell cycle arrest in the G2/M phase and suppresses cell division [1]. Yersinia pestis and Bacillus anthracis are effectively inhibited by ciprofloxacin lactate (Bay-09867), with MIC90s of 0.03 μg/mL and 0.12 μg/mL, respectively [2].
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ln Vivo |
In a mouse model of pneumonic plague, ciprofloxacin lactate (Bay-09867) (30 mg/kg; i.p.; 24 hours; BALB/c mice) is protective against Y. pestis [3]. By lowering LOX levels and raising MMP levels and activity, ciprofloxacin lactate (Bay-09867) (100 mg/kg; ig; daily for 4 weeks; C57BL/6J mice) enhances and speeds up aortic root enlargement. The frequency of aortic wall rupture and arterial dissection [4]. Ciprofloxacin (Bay-09867) Lactate (100 mg/kg; ir; daily for 4 weeks; C57BL/6J mice) causes mitochondrial malfunction, activation of cytoplasmic DNA sensor signaling, and DNA damage and release into the cytoplasm. Apoptosis and necroptosis in the aorta wall are increased by ciprofloxacin lactate [4].
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Cell Assay |
Cell Cycle Analysis[1]
Cell Types: Tenocytes Tested Concentrations: 5, 10, 20 and 50 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: diminished cellularity of tenocytes. Apoptosis analysis [1] Cell Types: Tenocytes Tested Concentrations: 50 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: The cell cycle was arrested in the G2/M phase and inhibited cell division of tenocytes. Western Blot Analysis [1] Cell Types: tenocytes Tested Concentrations: 50 μg/mL Incubation Duration: 0, 6, 12, 17 and 24 hrs (hours) Experimental Results: Down-regulated the expression of CDK-1 and cyclin B protein and mRNA. Upregulates the expression of PLK-1 protein. |
Animal Protocol |
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. |
References |
[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. |
Molecular Formula |
C20H24FN3O6
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Molecular Weight |
421.4195
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CAS # |
97867-33-9
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Related CAS # |
Ciprofloxacin;85721-33-1
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SMILES |
FC1C([H])=C2C(C(C(=O)O[H])=C([H])N(C2=C([H])C=1N1C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H])C1([H])C([H])([H])C1([H])[H])=O.O([H])C([H])(C(=O)O[H])C([H])([H])[H]
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
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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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3729 mL | 11.8646 mL | 23.7293 mL | |
5 mM | 0.4746 mL | 2.3729 mL | 4.7459 mL | |
10 mM | 0.2373 mL | 1.1865 mL | 2.3729 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.