| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| ln Vitro |
In the PAPE liposome experiment, Ecopladib reduced cPLA2α by 73% at 37 nM and inhibited sPLA2 by 16% at 1 μM. Ecopladib suppresses the generation of prostaglandins (PGF2α) and leukotrienes (LTB4 and LTC4/D4/E4) with an IC50 of 20−30 nM. Ecopladib is inactive against COX-1 and COX-2 at 20 μM and is over 100-fold the IC50 in MC-9 cells. Ecopladib inhibits 12- and 15-HETE, which are generated from arachidonic acid via the 12- and 15-lipoxygenase pathways, with an IC50 of around 0.3 μM [1].
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|---|---|
| ln Vivo |
In this model, ecopladib showed an ED50 of 8 mg/kg when taken orally, suggesting that it prevents the in vivo production of PGE2 produced from COX-2. Ecopladib administered orally effectively reduces paw edema caused by carrageenan; an ED50 of 40 mg/kg was found [1] based on a dose-response trial.
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| References | |
| Additional Infomation |
Ecopladib is an indole inhibitor of cytosolic phospholipase A2alpha (cPLA2alpha, type IVA phospholipase) with antiinflammatory activity.
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| Molecular Formula |
C39H33N2O5SCL3
|
|---|---|
| Molecular Weight |
748.11372
|
| Exact Mass |
746.118
|
| CAS # |
381683-92-7
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| PubChem CID |
204106
|
| Appearance |
White to off-white solid powder
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| Density |
1.35g/cm3
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| Boiling Point |
912.3ºC at 760 mmHg
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| Flash Point |
505.5ºC
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| Index of Refraction |
1.646
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| LogP |
10.692
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
50
|
| Complexity |
1150
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
FMMCHWHNSUBYAV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C39H33Cl3N2O5S/c40-30-14-18-36-33(24-30)32(20-22-49-31-15-12-29(13-16-31)39(45)46)37(19-21-43-50(47,48)25-26-11-17-34(41)35(42)23-26)44(36)38(27-7-3-1-4-8-27)28-9-5-2-6-10-28/h1-18,23-24,38,43H,19-22,25H2,(H,45,46)
|
| Chemical Name |
4-[2-[1-benzhydryl-5-chloro-2-[2-[(3,4-dichlorophenyl)methylsulfonylamino]ethyl]indol-3-yl]ethoxy]benzoic acid
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3367 mL | 6.6835 mL | 13.3670 mL | |
| 5 mM | 0.2673 mL | 1.3367 mL | 2.6734 mL | |
| 10 mM | 0.1337 mL | 0.6684 mL | 1.3367 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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