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| Targets |
Endothelial lipase and lipoprotein lipase. GSK-264220A is a potent endothelial lipase inhibitor with an IC50 of 16 nM. Endothelial lipase is a member of the triglyceride lipase gene family expressed in endothelial cells that prefers phospholipid substrates.
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| ln Vitro |
GSK-264220A inhibits endothelial lipase with an IC50 of 16 nM. It is also a lipoprotein lipase inhibitor. By inhibiting endothelial lipase, it may modulate lipid metabolism and reduce cardiovascular disease risk.
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| ln Vivo |
GSK-264220A has the potential to decrease the risk of cardiovascular disease. By blocking endothelial lipase activity, it may reduce the hydrolysis of phospholipids and modulate high-density lipoprotein (HDL) metabolism. Specific in vivo efficacy data are not detailed in the available literature.
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| Enzyme Assay |
In vitro enzyme inhibition assays for GSK-264220A involve measuring the activity of endothelial lipase in the presence of varying concentrations of the compound. The enzyme is incubated with a phospholipid substrate, and the release of fatty acids is quantified. The IC50 value is determined from the dose-response curve.
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| Cell Assay |
In vitro cell-based assays for GSK-264220A assess its effects on endothelial lipase activity in endothelial cells or other relevant cell types. Cells are treated with GSK-264220A, and lipase activity is measured. The compound's effects on lipid metabolism and cellular function can also be evaluated.
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| Animal Protocol |
Specific in vivo animal model protocols for GSK-264220A are not described in the available literature. To evaluate its in vivo efficacy, GSK-264220A could be administered to animal models of dyslipidemia or cardiovascular disease. Endpoints would include measurement of lipid profiles and markers of cardiovascular risk.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GSK-264220A are not reported in the available literature. As a small molecule inhibitor, its absorption, distribution, metabolism, and excretion properties would need to be characterized for in vivo use. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GSK-264220A are not available. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin and potential off-target effects.
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| References | |
| Additional Infomation |
GSK-264220A is a research tool for studying endothelial lipase function and lipid metabolism. It has the potential to decrease the risk of cardiovascular disease by modulating lipoprotein metabolism. The compound is not an approved therapeutic agent.
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| Molecular Formula |
C17H21N3O4S
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|---|---|
| Molecular Weight |
363.43
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| Exact Mass |
363.125
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| CAS # |
685506-42-7
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| PubChem CID |
2810413
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.633
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| LogP |
2.01
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
551
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LVOVQRPAMXCXTM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21N3O4S/c1-13-15(19-17(21)18-14-8-4-2-5-9-14)12-16(24-13)25(22,23)20-10-6-3-7-11-20/h2,4-5,8-9,12H,3,6-7,10-11H2,1H3,(H2,18,19,21)
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| Chemical Name |
1-(2-methyl-5-piperidin-1-ylsulfonylfuran-3-yl)-3-phenylurea
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| Synonyms |
GSK264220A; GSK 264220A; GSK-264220A
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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 : ≥ 100 mg/mL (~275.16 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.88 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 25.0 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: ≥ 2.5 mg/mL (6.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7516 mL | 13.7578 mL | 27.5156 mL | |
| 5 mM | 0.5503 mL | 2.7516 mL | 5.5031 mL | |
| 10 mM | 0.2752 mL | 1.3758 mL | 2.7516 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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