Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro. Clinafloxacin is against DNA gyrase and topoisomerase IV of S. aureus with IC 50 values of 0.92 μg/ml and 1.62 μg/ml, respectively.
性状
Solid
IC50 & Target[1][2]
Quinolone
体外研究(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 , gyr A mutant S. aureus and gyr A mutant S. aureus with MIC values of 0.016 μg/ml, 0.063 μg/ml and 0.915 μg/ml, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. 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.[2]. 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.
溶解度数据
In Vitro: DMSO : 2 mg/mL (5.47 mM; ultrasonic and warming and heat to 80°C)配制储备液