利福拉齐

生物活性靶点体外研究体内研究利福拉齐试剂级价格

利福拉齐

CAS号:129791-92-0
英文名:Rifalazil
中文名:利福拉齐
CBNumber:CB2437664
分子式:C51H64N4O13
分子量:941.07
MOL File:129791-92-0.mol

利福拉齐化学性质

熔点 :195-200° (dec)
沸点 :1065.6±65.0 °C(Predicted)
密度 :1.36±0.1 g/cm3(Predicted)
储存条件 :4°C, away from moisture
溶解度 :DMSO: 8.33 mg/mL (8.85 mM)
酸度系数(pKa) :4.28±0.70(Predicted)

利福拉齐性质、用途与生产工艺

生物活性 Rifalazil (ABI-1648; KRM-1648) 是利福霉素衍生物，可抑制细菌依赖 DNA 的 RNA 聚合酶 (RNA polymerase) 并阻断 RNA 聚合酶中的 β 亚基从而杀死细菌感染的细胞。Rifalazil (ABI-1648; KRM-1648) 是一种抗生素 (antibiotic)，对分枝杆菌，革兰氏阳性细菌，幽门螺杆菌，肺炎衣原体和沙眼衣原体有抑制作用，其 MIC 值在 0.00025 至 0.0025 μg/ml 之间。Rifalazil (ABI-1648; KRM-1648) 有潜力用于衣原体感染，梭菌相关性腹泻菌感染 (CDAD) 和结核病 (TB) 研究的相关研究。
靶点

IC50: RNA polymerase
体外研究

Rifalazil exhibits antimicrobal activity against Gram-positive enteric bacteria, inhibits Clostridium difficile , Clostridium perfringens , Bacteroides fragilis with MIC ₅₀ value of 0.0015, 0.0039, 0.0313 µg/ml, respectively. Rifalazil exhibits antimicrobal activity against Gram-negative enteric bacteria, inhibits Escherichia coli and Klebsiella pneumoniae with MIC ₅₀ value of 16 and 16 µg/ml, respectively. Rifalazil exhibits antimicrobal activity against non-enteric Gram-positive bacteria, inhibits Methicillin-susceptible Staphylococcus aureus , Methicillin-resistant S. aureus , Methicillin- and quinolone-resistant S. aureus , Staphylococcus epidermidis , Streptococcus pyogenes , Streptococcus pneumoniae with MIC ₅₀ value of 0.0078, 0.0078, 0.0078, 0.0078, 0.0002, 0.0001 µg/ml, respectively. Rifalazil exhibits antimicrobal activity against Helicobacter pylori , Chlamydia pneumoniae and Chlamydia trachomatis with MIC ₅₀ value of 0.004, 0.000125 and 0.00025 µg/ml, respectively.

体内研究

Rifalazil (oral gavage; 20, 25, and 150 mg/kg; 6-8 weeks) combines with isoniazid (INH) for 6 weeks or greater significantly reduced the number of mice per group in which M. tuberculosis is detected in both spleens and lungs compared to the reductions for the early and late controls. And the addition of Pyrazinamide (PZA) does not significantly improve RLZ-INH therapy at any time point.

Animal Model:	Female CD-1 mice infected with 5.2 × 10 ⁷ viable mycobacteria
Dosage:	20, 25, and 150 mg/kg; 6-8 weeks
Administration:	Oral gavage
Result:	Combined with isoniazid (INH) showed its potential for short-course treatment of Mycobacterium tuberculosis infection.