| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Bacterial DNA gyrase (topoisomerase II) and topoisomerase IV (inhibitor); DNA replication; fluoroquinolone antibacterial.
|
|---|---|
| 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].
Ciprofloxacin lactate inhibits bacterial DNA gyrase and topoisomerase IV, blocking DNA supercoiling and decatenation and causing DNA double-strand breaks. It is bactericidal and active against a broad spectrum of Gram-negative and Gram-positive pathogens, with MIC values typically in the 0.01–1 μg/mL range for susceptible strains. The lactate salt has similar antibacterial activity to ciprofloxacin hydrochloride. |
| 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].
In vivo, ciprofloxacin lactate is administered intravenously for severe infections, including complicated urinary tract infections, intra-abdominal infections and anthrax. It distributes widely to tissues and achieves therapeutic concentrations in plasma, urine and bile. Typical intravenous doses are 400 mg every 8–12 hours. |
| Enzyme Assay |
For DNA gyrase assays, purified bacterial gyrase is incubated with supercoiled DNA and ATP in the presence of serially diluted ciprofloxacin lactate (0.01–10 μg/mL). Supercoiling is analyzed by agarose gel electrophoresis, and IC50 is derived.
|
| 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. For antibacterial susceptibility testing, bacterial isolates are cultured in Mueller–Hinton broth and exposed to two-fold serial dilutions of ciprofloxacin lactate (0.001–16 μg/mL). The MIC is determined after 18–24 h, and time–kill assays assess bactericidal kinetics. |
| 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. For in vivo studies, mice with systemic or urinary tract infection receive ciprofloxacin lactate (e.g., 10–50 mg/kg, i.v. or oral), and bacterial burden in tissues is quantified by CFU counting. Plasma drug concentrations are measured by LC-MS/MS. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation The concentration of ciprofloxacin in breast milk is very low. Traditionally, fluoroquinolones (such as ciprofloxacin) are not recommended for use in infants due to concerns about adverse effects on the developing joints of infants. However, studies have shown that the risk is minimal. Calcium in breast milk may reduce the absorption of small amounts of fluoroquinolones in breast milk, but there is currently insufficient data to confirm or refute this claim. Breastfeeding women can use ciprofloxacin, but close monitoring of the infant's gut microbiota is necessary, for example, for changes in diarrhea or candidiasis (thrush, diaper rash). Avoiding breastfeeding for 3 to 4 hours after taking ciprofloxacin can reduce the amount of ciprofloxacin the infant is exposed to through breast milk. The risk to a breastfeeding infant from the mother's use of ear drops or eye drops containing ciprofloxacin is negligible. After using eye drops, to significantly reduce the amount of medication entering breast milk, press the tear duct near the corner of the eye for 1 minute or longer, then wipe away excess medication with absorbent tissue. ◉ Effects on breastfed infants A 2-month-old breastfed infant with a history of necrotizing enterocolitis developed pseudomembranous colitis, most likely due to the mother's self-treatment with ciprofloxacin. Ciprofloxacin was used as part of a multidrug regimen to treat three pregnant women with multidrug-resistant tuberculosis throughout pregnancy and postpartum. All three infants were breastfed (the extent and duration of breastfeeding were not specified). At 1.25, 1.8, and 3.9 years of age, all but one child showed normal development; the growth retardation was likely due to postnatal tuberculosis infection. ◉ Effects on breastfeeding and breast milk No relevant published information was found as of the revision date. |
| References |
|
| Molecular Formula |
C20H24FN3O6
|
|---|---|
| Molecular Weight |
421.4195
|
| Exact Mass |
403.154
|
| CAS # |
97867-33-9
|
| Related CAS # |
Ciprofloxacin;85721-33-1
|
| PubChem CID |
149514
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
656.4±55.0 °C at 760 mmHg
|
| Melting Point |
255-257ºC
|
| Flash Point |
350.8±31.5 °C
|
| Vapour Pressure |
0.0±2.1 mmHg at 25°C
|
| Index of Refraction |
1.624
|
| LogP |
0.04
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
631
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1C(=O)C2C(=CC(N3CCNCC3)=C(C=2)F)N(C2CC2)C=1)O.O=C(C(C)O)O
|
| InChi Key |
NRBJWZSFNGZBFQ-UHFFFAOYSA-N
|
| InChi Code |
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)
|
| Chemical Name |
1-cyclopropyl-6-fluoro-4-oxo-7-piperazin-1-ylquinoline-3-carboxylic acid;2-hydroxypropanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
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
|
|---|---|
| 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.) |
| 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.
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