| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Endothelial lipase inhibitor-1 targets endothelial lipase (EL, also known as LIPG), a member of the triglyceride lipase family that is primarily expressed in endothelial cells. EL hydrolyzes HDL phospholipids, reducing HDL particle size and promoting HDL clearance. Inhibition of EL increases HDL cholesterol levels and enhances reverse cholesterol transport, a key atheroprotective pathway.
|
|---|---|
| ln Vitro |
Endothelial lipase inhibitor-1 inhibits endothelial lipase activity in vitro. The compound binds to the active site of EL, preventing the hydrolysis of HDL phospholipids. In enzyme assays, the inhibitor shows potent activity with an IC50 in the low nanomolar to micromolar range depending on the assay conditions.
|
| ln Vivo |
In animal models, endothelial lipase inhibitor-1 increases plasma HDL cholesterol levels by inhibiting EL-mediated HDL hydrolysis. The compound may also affect other lipid parameters and has potential applications in the treatment of dyslipidemia and atherosclerosis. Detailed in vivo efficacy data are limited as the compound is a research tool.
|
| Enzyme Assay |
For endothelial lipase inhibition assays, recombinant human endothelial lipase is incubated with a fluorescent or radiolabeled phospholipid substrate (e.g., [³H]-phosphatidylcholine) and varying concentrations of the inhibitor. Enzyme activity is measured by the release of labeled free fatty acids or fluorescent products. IC50 values are calculated from dose-response curves.
|
| Cell Assay |
For cellular assays, endothelial cells (e.g., HUVECs) or cells expressing recombinant endothelial lipase are treated with the inhibitor at various concentrations. Lipase activity is measured by incubating cells with labeled HDL or phospholipid substrates and quantifying the release of labeled products. HDL binding, uptake, and cholesterol efflux may also be assessed.
|
| Animal Protocol |
In animal models, endothelial lipase inhibitor-1 is administered orally or intraperitoneally to evaluate its effects on plasma lipid levels. Blood samples are collected at various time points, and plasma HDL cholesterol, total cholesterol, and triglyceride levels are measured using enzymatic assays. Pharmacokinetic parameters are determined from plasma concentration-time data.
|
| ADME/Pharmacokinetics |
As a small-molecule inhibitor, endothelial lipase inhibitor-1 is expected to have oral bioavailability. The compound is likely metabolized in the liver via CYP450 enzymes and excreted in bile and urine. Pharmacokinetic parameters such as half-life, clearance, and volume of distribution would be determined in preclinical species.
|
| Toxicity/Toxicokinetics |
Endothelial lipase inhibitor-1 has demonstrated a favorable safety profile in preclinical studies. The compound is well-tolerated at effective doses. No significant toxicity has been reported. Standard preclinical toxicology studies would be required for therapeutic development.
|
| Additional Infomation |
Endothelial lipase inhibitor-1 is a small-molecule inhibitor of endothelial lipase (LIPG), an enzyme that hydrolyzes HDL phospholipids. By inhibiting EL, the compound increases HDL cholesterol levels and promotes reverse cholesterol transport, making it a potential therapeutic target for dyslipidemia and atherosclerosis.
|
| Molecular Formula |
C22H22N4O4
|
|---|---|
| Molecular Weight |
406.4345
|
| Exact Mass |
406.164
|
| CAS # |
1466427-02-0
|
| PubChem CID |
117926774
|
| Appearance |
Off-white to gray solid powder
|
| LogP |
2.3
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
30
|
| Complexity |
716
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1C[C@H](C2=C(C1)C(=CC=C2)OCC3=CC=CC=C3)NC(=O)C4=C(C(=O)NC(=O)N4)N
|
| InChi Key |
DZBXQBHHXZDUJS-MRXNPFEDSA-N
|
| InChi Code |
InChI=1S/C22H22N4O4/c23-18-19(25-22(29)26-20(18)27)21(28)24-16-10-4-9-15-14(16)8-5-11-17(15)30-12-13-6-2-1-3-7-13/h1-3,5-8,11,16H,4,9-10,12,23H2,(H,24,28)(H2,25,26,27,29)/t16-/m1/s1
|
| Chemical Name |
5-amino-2,4-dioxo-N-[(1R)-5-phenylmethoxy-1,2,3,4-tetrahydronaphthalen-1-yl]-1H-pyrimidine-6-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~61.51 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4604 mL | 12.3022 mL | 24.6045 mL | |
| 5 mM | 0.4921 mL | 2.4604 mL | 4.9209 mL | |
| 10 mM | 0.2460 mL | 1.2302 mL | 2.4604 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
