| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
MSSA(MIC= 0.3 µM);MRSA(MIC= 0.3-1µM);VISA(MIC= 0.3 µM)
PK150 targets bacterial cells, particularly Gram-positive bacteria. It is a Sorafenib analog with unique antibacterial properties. Its mechanism of action involves inhibiting bacterial growth at submicromolar concentrations. It shows activity against MSSA, MRSA, and VISA. |
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| ln Vitro |
In vitro, PK150 shows antibacterial activity against several pathogenic strains at submicromolar concentrations. It inhibits MSSA, MRSA, and VISA with MICs of 0.3, 0.3-1, and 0.3 µM, respectively. It also shows activity against vancomycin-resistant enterococci (MIC = 3 µM) and M. tuberculosis (MIC = 2 µM).
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| ln Vivo |
Using a mouse bloodstream infection model, the in vivo effectiveness of PK150 against methicillin-sensitive S. aureus (MSSA) (strain SH1000) is shown. The liver and heart have much lower bacterial loads when treated with PK150 (20 mg/kg; p.o.).In mice, PK150 (10 and 20 mg/kg orally; or 10 mg/kg intravenously) does not manifest any overt toxicity. For later therapeutic models, higher intravenous dosages of 20 mg/kg are avoided due to their severe toxic effects[1].
In vivo, PK150 shows oral bioavailability. As an orally bioavailable antibacterial agent, it can be administered to animal models of bacterial infection. Its ability to inhibit Gram-positive bacteria translates to in vivo efficacy in reducing bacterial burden. Detailed in vivo pharmacokinetic and efficacy studies are available from the compound's characterization. |
| Enzyme Assay |
In vitro antibacterial susceptibility testing for PK150 is performed using standardized methods such as broth microdilution. Various bacterial strains are cultured and exposed to serial dilutions of the compound. Minimum inhibitory concentrations (MIC) are determined as the lowest concentration that inhibits visible bacterial growth. The compound's activity is compared to other antibiotics.
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| Cell Assay |
For in vitro cell-based assays, bacterial cultures are treated with PK150 at various concentrations. Bacterial growth is monitored by measuring optical density at 600 nm. Time-kill curves can be generated to assess the bactericidal activity. The compound's effects on bacterial cell morphology can be examined by electron microscopy. Cytotoxicity in mammalian cells can be assessed using MTT or standard assays.
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| Animal Protocol |
Animal Model: Pathogen-free 9-week old female C57BL/6J mice[1]
Dosage: 20 mg/kg Administration: Administered p.o. Result: Both the liver and the heart had markedly decreased bacterial loads, which had decreased by about 100 times. In vivo animal studies with PK150 are conducted in models of bacterial infection. Animals are infected with pathogenic bacteria (e.g., S. aureus) and treated with the compound orally. Efficacy is measured by survival rates, bacterial clearance from tissues, and resolution of infection symptoms. Pharmacokinetic studies assess the compound's distribution, metabolism, and excretion. |
| ADME/Pharmacokinetics |
PK150 (CAS: 2165324-62-7) has a molecular weight of 394.68 g/mol and a molecular formula of C15H8ClF5N2O3. Appearance: solid powder. Purity: ≥98%. Solubility: DMSO (>25 mg/ml). Storage: -20°C. The compound is a Sorafenib analog with antibacterial activity.
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| Toxicity/Toxicokinetics |
PK150 is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As an antibacterial agent, it may have effects on normal bacterial flora. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicology studies would be required for therapeutic development.
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| References | |
| Additional Infomation |
PK150 is a Sorafenib analog with oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. It inhibits MSSA, MRSA, and VISA. It has the CAS number 2165324-62-7 and a molecular weight of 394.68 g/mol. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C15H8CLF5N2O3
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|---|---|
| Molecular Weight |
394.68
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| Exact Mass |
394.014
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| CAS # |
2165324-62-7
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| PubChem CID |
132190620
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
536
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C=C1NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)OC(O2)(F)F
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| InChi Key |
SHPYXCLUNMOJOB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H8ClF5N2O3/c16-10-3-1-7(5-9(10)14(17,18)19)22-13(24)23-8-2-4-11-12(6-8)26-15(20,21)25-11/h1-6H,(H2,22,23,24)
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| Chemical Name |
1-[4-chloro-3-(trifluoromethyl)phenyl]-3-(2,2-difluoro-1,3-benzodioxol-5-yl)urea
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| Synonyms |
PK-150
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~633.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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