| Size | Price | Stock | Qty |
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| Other Sizes |
| Targets |
Cadrofloxacin targets bacterial DNA gyrase and topoisomerase IV, which are essential enzymes for bacterial DNA replication, transcription, and repair. By inhibiting these enzymes, it prevents the supercoiling and uncoiling of DNA, leading to the inhibition of DNA synthesis and ultimately bacterial cell death. This mechanism is characteristic of the fluoroquinolone class of antibiotics.
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| ln Vitro |
In relation to Mycobacterium tuberculosis, ciprofloxacin has a MIC50 of 0.25 μg/mL[1]. Acinetobacter species are attacked by ciprofloxacin. The MIC90s of Stenotrophomonas maltophilia (Xanthomonas) and are, respectively, 0.03 and 2 μg/ml[2]. Cadrofloxacin inhibits the growth of Neisseria species, Moraxella catarrhalis, and Haemophilus influenzae. The MIC90 value is 0.06 μg/mL or less[2]. Cadrofloxacin is effective against Enterobacteriaceae family members, with a median MIC90 of 0.06 μg/mL and a range of 0.015 to 16 μg/mL [2].
In vitro, Cadrofloxacin is a potent, broad-spectrum fluoroquinolone. It is effective against aerobic and anaerobic Gram-positive and Gram-negative bacteria. Its activity is comparable to or better than other fluoroquinolones. It is being studied for its potential in managing antibiotic-resistant infections. Its spectrum of activity makes it a candidate for treating a variety of infections. |
| ln Vivo |
Rats' hepatic CYP2E1 activity is increased by cadefloxacin (9 mg/kg; ig; once or twice daily for 14 days) [2].
In vivo, Cadrofloxacin has shown efficacy in animal models of infection. As a fluoroquinolone, it is expected to be effective against systemic and localized bacterial infections. Its broad-spectrum activity suggests it could be used to treat respiratory, urinary tract, and skin infections. Its potency and effectiveness make it a promising agent for managing difficult-to-treat infections. |
| Enzyme Assay |
The in vitro activity of Cadrofloxacin is determined using standard antimicrobial susceptibility testing methods, such as broth microdilution or disk diffusion, according to CLSI guidelines. The minimum inhibitory concentration (MIC) is determined against a panel of bacterial strains, including both Gram-positive and Gram-negative organisms. The MIC90, the concentration required to inhibit 90% of isolates, is calculated.
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| Cell Assay |
Cadrofloxacin is a fluoroquinolone antibiotic, and its activity is typically assessed in bacterial culture. In a typical protocol, bacterial cells are cultured in broth and treated with varying concentrations of Cadrofloxacin. The optical density of the culture is measured to assess bacterial growth. The minimum bactericidal concentration (MBC) can also be determined by plating and counting colonies.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats, body weight 180-220 g[2]
Doses: 9 mg/kg Route of Administration: 1 or 2 times a day, Ig for 14 days Experimental Results: CYP2E1 mRNA expression in liver was enhanced, compared with the control group increased 1.6-fold, which was the same as the control rats. The level of CYP2E1 protein in liver microsomes was Dramatically higher than that of control rats, accounting for 190% of that of control rats. The in vivo efficacy of Cadrofloxacin is evaluated in animal models of infection, such as murine thigh infection or sepsis models. In these studies, animals are infected with a bacterial pathogen and then treated with Cadrofloxacin via oral or intravenous administration. The primary endpoint is the reduction in bacterial load in the target tissue (e.g., thigh, blood) compared to untreated controls. |
| ADME/Pharmacokinetics |
Cadrofloxacin has a molecular weight of 411.38 and a molecular formula of C₁₉H₂₀F₃N₃O₄. It is a synthetic fluoroquinolone antibiotic. As a fluoroquinolone, it is typically administered orally or intravenously. Its pharmacokinetic properties, including good oral bioavailability and tissue penetration, are characteristic of this class of antibiotics.
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| Toxicity/Toxicokinetics |
Cadrofloxacin, like other fluoroquinolones, has a toxicity profile that includes gastrointestinal disturbances, central nervous system effects, and potential for tendon damage. Its safety would be evaluated in preclinical and clinical studies. Its development as a therapeutic agent would require a careful assessment of its risk-benefit profile.
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| References |
[1]. Biedenbach DJ, et al. Antimicrobial activity of CS-940, a new trifluorinated quinolone. Antimicrob Agents Chemother. 1995 Oct;39(10):2325-30.
[2]. Bryskier A, et al. Fluoroquinolones and tuberculosis. Expert Opin Investig Drugs. 2002 Feb;11(2):233-58. |
| Additional Infomation |
Cadrofloxacin (Caderofloxacin, CS-940) is a novel fluoroquinolone antimicrobial agent. It has broad-spectrum activity against gram-positive and gram-negative bacteria, including aerobic and anaerobic species. It is being studied for the treatment of respiratory, urinary tract, and skin infections. It is not an approved drug and is a research compound for antibiotic development.
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| Molecular Formula |
C19H20F3N3O4
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|---|---|
| Molecular Weight |
411.3812
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| Exact Mass |
411.141
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| Elemental Analysis |
C, 55.47; H, 4.90; F, 13.85; N, 10.21; O, 15.56
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| CAS # |
153808-85-6
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| Related CAS # |
128427-55-4 (HCl);153808-85-6;
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| PubChem CID |
189912
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| Appearance |
Solid powder
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| Density |
1.458g/cm3
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| Boiling Point |
602.4ºC at 760mmHg
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| Flash Point |
318.1ºC
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| Vapour Pressure |
2.33E-15mmHg at 25°C
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| Index of Refraction |
1.588
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| LogP |
2.967
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
702
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(N2C3C(=CC(F)=C(N4CCNC(C)C4)C=3OC(F)F)C(=O)C(C(O)=O)=C2)CC1
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| InChi Key |
QBDBUKJBJJWZMG-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C19H20F3N3O4/c1-9-7-24(5-4-23-9)15-13(20)6-11-14(17(15)29-19(21)22)25(10-2-3-10)8-12(16(11)26)18(27)28/h6,8-10,19,23H,2-5,7H2,1H3,(H,27,28)/t9-/m0/s1
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| Chemical Name |
1-cyclopropyl-8-(difluoromethoxy)-6-fluoro-7-[(3S)-3-methylpiperazin-1-yl]-4-oxoquinoline-3-carboxylic acid
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| Synonyms |
CS940; CS 940; CS-940
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| HS Tariff Code |
2934.99.9001
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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 Vitro) |
DMSO : ~10 mg/mL (~24.31 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4308 mL | 12.1542 mL | 24.3084 mL | |
| 5 mM | 0.4862 mL | 2.4308 mL | 4.8617 mL | |
| 10 mM | 0.2431 mL | 1.2154 mL | 2.4308 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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