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Cat. No.: HY-U00037

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Ecopladib

Name: Ecopladib
Brand: MedChemExpress
SKU: HY-U00037
Price: 1420.00 USD
Availability: PreOrder

(Synonyms: PLA 725)

Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC₅₀s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.

For research use only. We do not sell to patients.

CAS No.: 381683-92-7
Formula: C₃₉H₃₃Cl₃N₂O₅S
Molecular Weight:748.11

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Ecopladib Chemical Structure

CAS No.: 381683-92-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC₅₀s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.

IC₅₀ & Target

IC50: 0.15 μM (cPLA2α, in GLU micelle), 0.11 μM (cPLA2α, rat blood)^[1]

All Phospholipase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MC9	IC₅₀	20 nM Compound: 123, ecopladib	Inhibition of LTB4 production in mouse MC9 cells Inhibition of LTB4 production in mouse MC9 cells	[PMID: 17305324]
MC9	IC₅₀	20 nM Compound: 123, ecopladib	Inhibition of LTC4 production in mouse MC9 cells Inhibition of LTC4 production in mouse MC9 cells	[PMID: 17305324]
MC9	IC₅₀	20 nM Compound: 123, ecopladib	Inhibition of LTD4 production in mouse MC9 cells Inhibition of LTD4 production in mouse MC9 cells	[PMID: 17305324]
MC9	IC₅₀	20 nM Compound: 123, ecopladib	Inhibition of LTE4 production in mouse MC9 cells Inhibition of LTE4 production in mouse MC9 cells	[PMID: 17305324]
MC9	IC₅₀	20 nM Compound: 123, ecopladib	Inhibition of PGF2-alpha production in mouse MC9 cells Inhibition of PGF2-alpha production in mouse MC9 cells	[PMID: 17305324]

In Vitro

Ecopladib inhibits cPLA2α in the PAPE liposome assay at 73% at a concentration of 37 nM, while it inhibits sPLA2 at 16% at 1 μM. Ecopladib inhibits the production of prostaglandins (PGF2α) and leukotrienes (LTB4 and LTC4/D4/E4) with comparable IC₅₀s of 20?30 nM. Ecopladib is inactive against COX-1 and COX-2 at 20 μM, which is nearly 100 times the IC₅₀ in the MC-9 cells. Ecopladib inhibit 12- and 15-HETE, which are derived from arachidonic acid via the 12- and 15-lipoxygenase pathways and the IC₅₀s are ～0.3 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

In Vivo

Ecopladib is orally efficacious in this model and displays an ED₅₀ of 8 mg/kg, demonstrating that it can inhibit COX-2 derived PGE2 formation in vivo. Ecopladib is orally efficacious at reducing carrageenan-induced paw swelling:?from dose?response studies, it is determined that the ED₅₀ is 40 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 381683-92-7
Appearance Solid
Molecular Weight 748.11
Formula C₃₉H₃₃Cl₃N₂O₅S
Color White to off-white
SMILES

O=C(O)C1=CC=C(OCCC2=C(CCNS(=O)(CC3=CC=C(Cl)C(Cl)=C3)=O)N(C(C4=CC=CC=C4)C5=CC=CC=C5)C6=C2C=C(Cl)C=C6)C=C1
Synonyms

PLA 725
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lee KL, et al. Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha. J Med Chem. 2007 Mar 22;50(6):1380-400. Epub 2007 Feb 17. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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