| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as platelet-activating factor acetylhydrolase. Lp-PLA2 is a phospholipase A2 enzyme that is involved in the hydrolysis of phospholipids or lipoprotein lipids. It is transported by low-density lipoprotein (LDL) and rapidly cleaves oxidized phosphatidylcholine molecules that result from LDL oxidation. Lp-PLA2 has been implicated in the pathogenesis of atherosclerosis and Alzheimer's disease, making it a therapeutic target for these conditions.
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| ln Vitro |
Phospholipase A2 that is involved in the hydrolysis of phospholipids or lipoprotein lipids is known as lipoprotein-associated phospholipase A2 (Lp-PLA2). Low-density lipoprotein (LDL) is moved by Lp-PLA2, which then quickly cleaves oxidized phosphatidylcholine molecules that result from LDL oxidation[1].
GSK2814338 is a potent inhibitor of Lp-PLA2 enzyme activity. As an Lp-PLA2 inhibitor, it blocks the hydrolysis of oxidized phospholipids in LDL, thereby reducing the production of pro-inflammatory mediators such as lysophosphatidylcholine and oxidized non-esterified fatty acids. Specific IC50 values for Lp-PLA2 inhibition are not detailed in the available literature, but the compound is described as a "novel and potent" inhibitor with potential for atherosclerosis and Alzheimer's disease research. |
| ln Vivo |
Specific in vivo activity data for GSK2814338 are not extensively reported in the available literature. As an Lp-PLA2 inhibitor, it would be expected to reduce inflammation and oxidative stress in vivo by inhibiting the production of pro-inflammatory mediators from oxidized LDL. The compound has potential for studying atherosclerosis and Alzheimer's disease in animal models.
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| Enzyme Assay |
In vitro enzyme inhibition assays for GSK2814338 involve measuring the activity of Lp-PLA2 in the presence of varying concentrations of the compound. The enzyme is incubated with a phospholipid substrate, and the release of fatty acids or other hydrolysis products is quantified. The IC50 value is determined from the dose-response curve. These protocols are typically referenced from primary literature and are for research use only.
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| Cell Assay |
In vitro cell-based assays for GSK2814338 can be performed in cell types relevant to atherosclerosis and Alzheimer's disease, such as macrophages or neuronal cells. Cells are treated with GSK2814338, and the levels of inflammatory markers or oxidized lipid products are measured. The compound's effects on cellular function and viability can also be evaluated using standard cell viability assays such as MTT or CellTiter-Glo.
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| Animal Protocol |
Specific in vivo animal model protocols for GSK2814338 are not described in the available literature. To evaluate its in vivo efficacy, GSK2814338 could be administered to animal models of atherosclerosis (such as ApoE-deficient mice) or Alzheimer's disease. Endpoints would include measurement of inflammatory markers, lipid profiles, and pathological changes in relevant tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GSK2814338 are not extensively reported in the available literature. As a small molecule inhibitor with a molecular weight of 468.38 and a LogP of 3.4, it is expected to have reasonable oral bioavailability and tissue penetration. The compound is supplied as a white to off-white solid powder and is typically stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GSK2814338 are not available in the searched literature. 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 prior to any clinical application. The compound is for research use only and not for human use.
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| References | |
| Additional Infomation |
GSK2814338 is a research tool for studying Lp-PLA2 function and its role in inflammatory diseases. Lp-PLA2 has been identified as a potential therapeutic target for atherosclerosis and Alzheimer's disease. The compound is also known as Lp-PLA2-IN-1. It is not an approved therapeutic agent and is intended for research use only.
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| Molecular Formula |
C21H17F5N4O3
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|---|---|
| Molecular Weight |
468.3767
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| Exact Mass |
468.122
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| Elemental Analysis |
C, 53.85; H, 3.66; F, 20.28; N, 11.96; O, 10.25
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| CAS # |
1420367-28-7
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| PubChem CID |
71236597
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| Appearance |
White to off-white solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
780
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCCN2C1=CC(=NC2=O)OCC3=CC(=C(C(=C3)F)OC4=CN=C(C=C4)C(F)(F)F)F
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| InChi Key |
QJIGPJZJKXZSNF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17F5N4O3/c1-29-5-2-6-30-18(29)9-17(28-20(30)31)32-11-12-7-14(22)19(15(23)8-12)33-13-3-4-16(27-10-13)21(24,25)26/h3-4,7-10H,2,5-6,11H2,1H3
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| Chemical Name |
8-[[3,5-difluoro-4-[6-(trifluoromethyl)pyridin-3-yl]oxyphenyl]methoxy]-1-methyl-3,4-dihydro-2H-pyrimido[1,2-c]pyrimidin-6-one
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| Synonyms |
GSK-2814338 GSK2814338 Lp-PLA2 -IN-1
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| HS Tariff Code |
2934.99.03.00
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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) |
Ethanol : ~25 mg/mL (~53.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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 (5.34 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1350 mL | 10.6751 mL | 21.3502 mL | |
| 5 mM | 0.4270 mL | 2.1350 mL | 4.2700 mL | |
| 10 mM | 0.2135 mL | 1.0675 mL | 2.1350 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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