Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Purity: ≥98%
Clinafloxacin HCl (also known as CI-960, PD127391, AM-1091), the hydrochloride salt of Clinafloxacin, is an investigational, broad-spectrum fluoroquinolone class of antibiotic that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumonia. The quinolone carboxylic acid class of broad-spectrum antibiotics is presently being developed for oral and intravenous treatment of serious infections. With strong broad-spectrum in vitro activity against gram-positive, gram-negative, and anaerobic pathogens, clinafloxacin is a novel fluoroquinolone antibiotic.
Targets |
Topoisomerase IV; DNA gyrase
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ln Vitro |
Clinafloxacin shows efficacy against S. pneumonia in parC-gyrA mutants, with a minimum inhibitory concentration (MIC) of 1 μg/ml[2].
Clinafloxacin hydrochloride possesses antibacterial properties against S. aureus mutant strains with altered targets. It has MIC values of 0.016 µg/ml, 0.063 µg/ml, and 0.915 µg/ml against wild type S. aureus, gyrA mutant S. aureus, and gyrA mutant S. aureus, respectively[3]. |
ln Vivo |
Clinafloxacin pneumococcal meningitis that is resistant to penicillin responds well to clinafloxacin therapy in the rabbit model.
Clinafloxacin produces an initial reduction at 6 hours when used with the CS strain (2349) (Clinafloxacin MIC=0.12 μg/ml) at doses of 10 mg/kg and 20 mg/kg. The final reduction in mean log cfu/ml at 24 hours is 22.30 and 23.83, respectively. Both are bactericidal at this point, but show regrowth at that time. But in this meningitis model in rabbits, even at 20 mg/kg per day, clinafloxacin (MIC=0.5 μg/ml) does not reduce bacterial titers[3]. This is because the CR strain (4371) exhibits this property. |
References |
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Molecular Formula |
C17H18CL2FN3O3
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Molecular Weight |
402.24752
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Exact Mass |
401.07
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Elemental Analysis |
C, 50.76; H, 4.51; Cl, 17.63; F, 4.72; N, 10.45; O, 11.93
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CAS # |
105956-99-8
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Related CAS # |
105956-97-6; 105956-99-8 (HCl)
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Appearance |
Solid powder
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SMILES |
C1CC1N2C=C(C(=O)C3=CC(=C(C(=C32)Cl)N4CCC(C4)N)F)C(=O)O.Cl
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InChi Key |
BMACYHMTJHBPOX-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C17H17ClFN3O3.ClH/c18-13-14-10(5-12(19)15(13)21-4-3-8(20)6-21)16(23)11(17(24)25)7-22(14)9-1-2-9;/h5,7-9H,1-4,6,20H2,(H,24,25);1H
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Chemical Name |
7-(3-aminopyrrolidin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid;hydrochloride
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Synonyms |
CI-960; PD-127391; AM-109; CI960; PD127391; AM109; Clinafloxacin hydrochloride; Clinafloxacin HCl; CI-960 HCl; UNII-G17M59V0FY ;CI 960 HCl
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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) |
5%TFA: ~3.02 mg/mL
DMSO: ~0.03 mg/mL (~0.08 mM) |
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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.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4860 mL | 12.4301 mL | 24.8602 mL | |
5 mM | 0.4972 mL | 2.4860 mL | 4.9720 mL | |
10 mM | 0.2486 mL | 1.2430 mL | 2.4860 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.
Antimicrob Agents Chemother . 2001 Dec;45(12):3544-7. td> |