PK150

Research use only, not for human use.

PK150 shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations.

PK150 shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations.

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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 miceDosage: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 oldDosage: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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Others

Other Targets

others

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2165324-62-7

394.68

C15H3ClF5N2O3

>98% (HPLC)

DMSO:250 mg/mL (633.42 mM; Need ultrasonic)

O=C(Nc1ccc2c(c1)OC(F)(F)O2)Nc1ccc(Cl)c(C(F)(F)F)c1

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(-20℃)

With Ice Pack

≥ 2 years