产品
编 号：F116801
分子式：C18H21FN2O6S
分子量：412.43
分子式：C18H21FN2O6S
分子量：412.43
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 1312473-63-4
产品详情
生物活性：
PF-5081090 (LpxC-4) is a potent LpxC inhibitor, is a rapidly bactericidal with broad-spectrum activity. PF-5081090 serves as a regulator of lipid A biosynthesis in Gram-negative pathogens.
体内研究：
PF-5081090 (8.75, 75, 300 mg/kg; s.c.; single dose) exhibits a exposure increasing in linear manner across the dose range in mice, with area under the concentration-time curve (AUC) and maximum concentration of drug in serum (Cmax) increasing with a proportional increase in dose.PF-5081090 shows potent efficacies against sentinel strains of P. aeruginosa and K. pneumoniain CD-1 mice, with effective dose (ED50) ranging from 7.4-55.9 mg/kg (against acute septicemia model), <25 mg/kg (against pneumonia model), and 16.8 mg/kg (against neutropenic thigh model) in mice infected with P. aeruginosa PA-1950.Pharmacokinetics of PF-5081090 in CD-1 miceaDose (mg/kg)Cmax (mg/L)Tmax (h)AUC (h?mg/L)Free AUC (h?mg/L)T1/2 (h)CL (L/h/kg)Vss (L/kg)
18.755.020.255.091.580.63.792.20
7515.500.3317.605.460.694.323.30
30075.400.3376.3023.700.683.922.53
a Following single subcutaneous doses.
体外研究：
PF-5081090 shows strong potency against a broad spectrum of Gram-negative pathogens with IC50s of 1.1 nM (P. aeruginosa), 0.069 nM (K. pneumonia) and MIC90s of 1 μg/mL (P. aeruginosa, K. pneumoniae), 0.25 μg/mL (E. coli), 0.5 μg/mL (Enterobacter spp), 2 μg/mL (S. maltophilia).PF-5081090 (0.25 μg/mL; 0-50 h) demonstrates sustained bactericidal activities against P. aeruginosa UC12120 (A), PA-1955 (B), and K. pneumoniae KP-1487.PF-5081090 (32 mg/L) increases antibiotic susceptibility in Acinetobacter baumannii with rifampicin, vancomycin, azithromycin, imipenem and amikacin.PF-5081090 (32 mg/L) inhibits lipid A biosynthesis, and significantly increases cell permeability in A. baumannii.
PF-5081090 (LpxC-4) is a potent LpxC inhibitor, is a rapidly bactericidal with broad-spectrum activity. PF-5081090 serves as a regulator of lipid A biosynthesis in Gram-negative pathogens.
体内研究：
PF-5081090 (8.75, 75, 300 mg/kg; s.c.; single dose) exhibits a exposure increasing in linear manner across the dose range in mice, with area under the concentration-time curve (AUC) and maximum concentration of drug in serum (Cmax) increasing with a proportional increase in dose.PF-5081090 shows potent efficacies against sentinel strains of P. aeruginosa and K. pneumoniain CD-1 mice, with effective dose (ED50) ranging from 7.4-55.9 mg/kg (against acute septicemia model), <25 mg/kg (against pneumonia model), and 16.8 mg/kg (against neutropenic thigh model) in mice infected with P. aeruginosa PA-1950.Pharmacokinetics of PF-5081090 in CD-1 miceaDose (mg/kg)Cmax (mg/L)Tmax (h)AUC (h?mg/L)Free AUC (h?mg/L)T1/2 (h)CL (L/h/kg)Vss (L/kg)
18.755.020.255.091.580.63.792.20
7515.500.3317.605.460.694.323.30
30075.400.3376.3023.700.683.922.53
a Following single subcutaneous doses.
体外研究：
PF-5081090 shows strong potency against a broad spectrum of Gram-negative pathogens with IC50s of 1.1 nM (P. aeruginosa), 0.069 nM (K. pneumonia) and MIC90s of 1 μg/mL (P. aeruginosa, K. pneumoniae), 0.25 μg/mL (E. coli), 0.5 μg/mL (Enterobacter spp), 2 μg/mL (S. maltophilia).PF-5081090 (0.25 μg/mL; 0-50 h) demonstrates sustained bactericidal activities against P. aeruginosa UC12120 (A), PA-1955 (B), and K. pneumoniae KP-1487.PF-5081090 (32 mg/L) increases antibiotic susceptibility in Acinetobacter baumannii with rifampicin, vancomycin, azithromycin, imipenem and amikacin.PF-5081090 (32 mg/L) inhibits lipid A biosynthesis, and significantly increases cell permeability in A. baumannii.
产品资料
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