| 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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| Other Sizes |
Purity: ≥98%
| Targets |
The primary target of EA4 is rPLA2 (red blood cell phospholipase A2), a calcium-dependent cytosolic phospholipase A2 (cPLA2). EA4 inhibits the ionophore-induced arachidonic acid release from human and bovine red blood cells, indicating that rPLA2 is responsible for the Ca2+-dependent release of arachidonic acid from mammalian RBCs. By inhibiting rPLA2, EA4 blocks the production of arachidonic acid and its downstream metabolites.
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| ln Vitro |
rPLA2 and cPLA2 are inhibited by EA4 (9 μM, 24 μM)[1]. EA4 has a 130 μM Ki value that inhibits rPLA2 [1]. In a time-regulated manner, EA4 (50 μM) strongly suppresses the release of AA from light erythrocytes caused by A23187 [1].
EA4 inhibits rPLA2 with a Ki value of 130 μM. It inhibits the ionophore-induced arachidonic acid release from human and bovine red blood cells. This demonstrates that rPLA2 is responsible for the Ca2+-dependent release of arachidonic acid from mammalian RBCs. EA4 can be used for research on hemostasis, thrombosis, and erythropoiesis. |
| ln Vivo |
In vivo activity data for EA4 are not detailed in the available sources. The compound's primary characterization comes from in vitro enzyme inhibition assays using purified rPLA2 and red blood cell-based assays. Specific in vivo efficacy studies have not been described in the available literature. The compound is used as a tool to study the role of rPLA2 in cellular processes.
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| Enzyme Assay |
The rPLA2 inhibition assay measures the enzymatic activity of purified rPLA2 using a labeled substrate, such as 1-palmitoyl-2-[¹⁴C]arachidonyl-phosphatidylcholine. The enzyme is incubated with the substrate in the presence of Ca2+ and varying concentrations of EA4. The reaction is terminated, and the released [¹⁴C]-arachidonic acid is extracted and quantified by liquid scintillation counting. The Ki value is calculated from the inhibition curve using appropriate enzyme kinetics models.
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| Cell Assay |
To evaluate the effect of EA4 on arachidonic acid release, human or bovine red blood cells are loaded with [³H]-arachidonic acid and stimulated with a calcium ionophore (e.g., A23187) to induce arachidonic acid release. EA4 is added at various concentrations before stimulation. After incubation, the amount of [³H]-arachidonic acid released into the supernatant is measured by liquid scintillation counting. The percentage inhibition of arachidonic acid release is calculated.
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| Animal Protocol |
Specific in vivo animal experiment protocols for EA4 are not detailed in the available sources. The compound has not been described in the context of animal models of thrombosis or other diseases. Given its in vitro activity as a rPLA2 inhibitor, it may be evaluated in animal models of hemostasis or thrombosis, but such data are not currently available.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for EA4 are not provided in the available sources. The compound is a small molecule with a molecular weight of approximately 354.8 (based on its formula C19H17ClN2O2). Standard pharmacokinetic studies would typically involve administering the compound to rodents and measuring plasma concentrations over time using LC-MS/MS to determine key PK parameters, but such data are not currently available.
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| Toxicity/Toxicokinetics |
Specific toxicity data for EA4 are not provided in the available sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
EA4 is a quinone derivative that inhibits rPLA2 with a Ki of 130 μM. Its chemical name is 7-chloro-6-[4-(diethylamino)phenyl]quinoline-5,8-dione. The compound has a CAS number of 389614-94-2. EA4 inhibits the ionophore-induced arachidonic acid release from human and bovine red blood cells, indicating that rPLA2 is responsible for the Ca2+-dependent release of arachidonic acid from mammalian RBCs. It is supplied for research purposes.
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| Molecular Formula |
C19H17N2O2CL
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|---|---|
| Molecular Weight |
340.80348
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| Exact Mass |
340.097
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| CAS # |
389614-94-2
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| PubChem CID |
10042917
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| Appearance |
Light blue to blue solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
508.3±50.0 °C at 760 mmHg
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| Flash Point |
261.2±30.1 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.634
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| LogP |
4.42
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
534
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XAZVKSMDPVMMPP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17ClN2O2/c1-3-22(4-2)13-9-7-12(8-10-13)15-16(20)19(24)17-14(18(15)23)6-5-11-21-17/h5-11H,3-4H2,1-2H3
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| Chemical Name |
7-chloro-6-[4-(diethylamino)phenyl]-5,8-quinolinedione
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| Synonyms |
EA4; EA 4; EA-4
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~50 mg/mL (~146.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.93 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (2.93 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 10.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9343 mL | 14.6714 mL | 29.3427 mL | |
| 5 mM | 0.5869 mL | 2.9343 mL | 5.8685 mL | |
| 10 mM | 0.2934 mL | 1.4671 mL | 2.9343 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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