1. Anti-infection
  2. Bacterial
  3. PK150

PK150 

Cat. No.: HY-133119 Purity: 99.37%
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

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5337 mL 12.6685 mL 25.3370 mL
5 mM 0.5067 mL 2.5337 mL 5.0674 mL
10 mM 0.2534 mL 1.2668 mL 2.5337 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PK150PK 150PK-150BacterialantibacterialGram-positiveMSSAMRSAVISAInhibitorinhibitorinhibit

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Product Name:
PK150
Cat. No.:
HY-133119
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