Clinafloxacin

Additional information:
Clinafloxacin (free base) is an investigational fluoroquinolone antibiotic. Despite its promising antibiotic activity, the clinical development of clinafloxacin has been hampered by its risk for inducing serious side effects.|Product information|CAS Number: 105956-97-6|Molecular Weight: 365.79|Formula: C17H17ClFN3O3|Synonym:|PD127391|PD 127391|PD-127391|AM-1091|CI-960|Chemical Name: 7-(3-aminopyrrolidin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid|Smiles: NC1CN(CC1)C1=C(Cl)C2=C(C=C1F)C(=O)C(=CN2C1CC1)C(O)=O|InChiKey: QGPKADBNRMWEQR-UHFFFAOYSA-N|InChi: InChI=1S/C17H17ClFN3O3/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)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 2 mg/mL (5.ICAM-5 Protein, Mouse (HEK293, His) Purity 47 mM; ultrasonic and warming and heat to 80°C)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:31536279 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|Clinafloxacin exhibits activity against S. pneumonia with an MIC of 1μg/ml for the parC-gyrA mutants. Clinafloxacin hydrochloride has antibacterial activities against target-altered mutant strains of S. aureus. It against Wild type S. aureus, gyrA mutant S. aureus and gyrA mutant S. aureus with MIC values of 0.016 µg/ml, 0.063 µg/ml and 0.915 µg/ml, respectively.|In Vivo:|Clinafloxacin is very effective for the therapy of penicillin-resistant, ciprofloxacin-susceptible pneumococcal meningitis in the rabbit model. With the CS strain (2349)(Clinafloxacin MIC=0.12 μg/ml), at a dose of 10 mg/kg and 20 mg/kg per day Clinafloxacin achieves an initial reduction at 6 hr. Both are bactericidal at this point but presents regrowth at 24 hr, and the final reduction at 24 hr in mean log cfu/ml is 22.30 and 23.83, respectively. However, With the CR strain (4371)(Clinafloxacin MIC=0.5 μg/ml), Clinafloxacin even at 20 mg/kg per day does not decrease bacterial titers at any time point in this rabbit model of meningitis.|References:|M Takei, et al. Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition.Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.Randa H Abdelkreem, et al. DNA Gyrase and Topoisomerase IV Mutations and their effect on Quinolones Resistant Proteus mirabilis among UTIs Patients. Pak J Med Sci. Sep-Oct 2020;36(6):1234-1240.A Domenech, et al. Experimental study of clinafloxacin alone and in combination in the treatment of ciprofloxacin-susceptible and -resistant pneumococcal meningitis.Microb Drug Resist. 2003;9 Suppl 1:S53-9.Products are for research use only. Not for human use.|