盐酸克林沙星

生物活性靶点体外研究体内研究盐酸克林沙星试剂级价格

盐酸克林沙星

CAS号:105956-99-8
英文名:Clinafloxacin hydrochloride
中文名:盐酸克林沙星
CBNumber:CB3148235
分子式:C17H18Cl2FN3O3
分子量:402.25
MOL File:105956-99-8.mol

盐酸克林沙星化学性质

熔点 :162-168°C
储存条件 :Refrigerator
溶解度 :DMSO (Slightly), Methanol (Slightly), Water (Slightly, Heated)
形态 :Solid
颜色 :Pale Yellow to Light Yellow
稳定性 :Hygroscopic

盐酸克林沙星性质、用途与生产工艺

生物活性 Clinafloxacin hydrochloride (AM 1091 hydrochloride) 是一种高效广谱氟喹诺酮类抗生素 (antibiotic)，对革兰氏阳性、革兰氏阴性和厌氧病原体均有抑制活性。Clinafloxacin hydrochloride 对金黄色葡萄球菌的DNA促旋酶 (DNA gyrase) 和拓扑异构酶 IV (topoisomerase IV) 有抑制作用，IC50 值分别为 0.92 µg/ml 和 1.62 µg/ml。
靶点

MIC: 1 μg/ml (parC-gyrA mutants, S. pneumonia )
体外研究

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.
体内研究

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.