1. Anti-infection
  2. Bacterial
  3. PK150

PK150 

Cat. No.: HY-133119
Handling Instructions

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.

For research use only. We do not sell to patients.

PK150 Chemical Structure

PK150 Chemical Structure

CAS No. : 2165324-62-7

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Description

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[1].

IC50 & Target

MIC: 0.3 µM (MSSA), 0.3-1 µM (MRSA), 0.3 µM (VISA)[1]

In Vivo

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[1].
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[1].

Animal Model: Pathogen-free 9-week old female C57BL/6J mice[1]
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[1]
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.
Molecular Weight

394.68

Formula

C₁₅H₈ClF₅N₂O₃

CAS No.

2165324-62-7

SMILES

O=C(NC1=CC=C(OC(F)(F)O2)C2=C1)NC3=CC=C(Cl)C(C(F)(F)F)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PK150PK 150PK-150BacterialantibacterialGram-positiveMSSAMRSAVISAInhibitorinhibitorinhibit

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