产品
编 号：F563931
分子式：C15H8ClF5N2O3
分子量：394.68
分子式：C15H8ClF5N2O3
分子量：394.68
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 2165324-62-7
产品详情
生物活性：
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 μM, respectively.
体内研究：
The in vivo efficacy of PK150 against methicillin-sensitive S. aureus (MSSA) (strain SH1000) is demonstrated in a murine bloodstream infection model. PK150 (20?mg/kg; p.o.) significantly reduces bacterial loads in the liver and heart.PK150 (10 and 20mg/kg orally; or 10mg/kg intravenously) shows no obvious signs of toxicity in mice. Higher i.v. dosing of 20mg/kg results in severe toxic effects and is thus avoided for subsequent therapeutic models.Animal Model:Pathogen-free 9-week old female C57BL/6J mice
Dosage:20?mg/kg
Administration:Administered p.o.
Result:Bacterial loads in the liver and heart were both significantly reduced by approximately 100-fold.
Animal Model:Outbred male CD-1 mice, 4 weeks old
Dosage:10 and 20 mg/kg (Pharmacokinetic Analysis)
Administration:Administered by intragastric gavage at 10 and 20 mg/kg or intravenously at 10 mg/kg
Result:Oral bioavailability was approximately 63% and the mean residence time was slightly enhanced via this administration route.T1/2=11.69±1.5, 9.67±0.2, and 9.37±0.5 hours for 10 mg/kg i.v., 10 mg/kg p.o., and 20 mg/kg p.o., respectively.
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 μM, respectively.
体内研究：
The in vivo efficacy of PK150 against methicillin-sensitive S. aureus (MSSA) (strain SH1000) is demonstrated in a murine bloodstream infection model. PK150 (20?mg/kg; p.o.) significantly reduces bacterial loads in the liver and heart.PK150 (10 and 20mg/kg orally; or 10mg/kg intravenously) shows no obvious signs of toxicity in mice. Higher i.v. dosing of 20mg/kg results in severe toxic effects and is thus avoided for subsequent therapeutic models.Animal Model:Pathogen-free 9-week old female C57BL/6J mice
Dosage:20?mg/kg
Administration:Administered p.o.
Result:Bacterial loads in the liver and heart were both significantly reduced by approximately 100-fold.
Animal Model:Outbred male CD-1 mice, 4 weeks old
Dosage:10 and 20 mg/kg (Pharmacokinetic Analysis)
Administration:Administered by intragastric gavage at 10 and 20 mg/kg or intravenously at 10 mg/kg
Result:Oral bioavailability was approximately 63% and the mean residence time was slightly enhanced via this administration route.T1/2=11.69±1.5, 9.67±0.2, and 9.37±0.5 hours for 10 mg/kg i.v., 10 mg/kg p.o., and 20 mg/kg p.o., respectively.
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