Efipladib
Efipladib is a potent, selective and orally active cPLA2α inhibitor with an IC50 of 0.04 μM and a Kd of 0.067 μM.
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- No. CAS: 381683-94-9
- Fòrmula: C40H35Cl3N2O4S
- Peso molecular:746.14
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
cPLA2α 0.04 μM (IC50) |
cPLA2α 0.067 μM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MC9 | IC50 |
0.02 μM
Compound: 111
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Inhibition of LTB4 production in mouse MC9 cells
Inhibition of LTB4 production in mouse MC9 cells
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[PMID: 18498150] |
| MC9 | IC50 |
0.02 μM
Compound: 111
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Inhibition of PGF2alpha production in mouse MC9 cells
Inhibition of PGF2alpha production in mouse MC9 cells
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[PMID: 18498150] |
| MC9 | IC50 |
0.9 μM
Compound: 111
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Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells
Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells
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[PMID: 18498150] |
| U-937 | IC50 |
0.00054 μM
Compound: 1
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Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting
Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting
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[PMID: 25102418] |
| U-937 | IC50 |
0.54 nM
Compound: 1
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Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting
Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting
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[PMID: 25102418] |
In Vitro
Efipladib (10-25 μM; 24-72 h) increases COX-1 and PGE2 levels in PC3 and LNCaP cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 and LNCaP cells
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Concentration:10, 15, 20 and 25 μM
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Incubation Time:72 h
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Result:Significantly decreased cPLA2α activity. Increased COX-1 protein levels. Increased COX-2 protein levels in PC3 cells.
In Vivo
Efipladib (100 mg/kg; p.o.; once) significantly inhibits the nociceptive response 1 h after administration in the rat Complete Freund’s Adjuvant (CFA) nociception model[2].
Efipladib is unable to cross the BBB to gain access to the central compartment[2].
Efipladib (100 nM; IT; 5 μL) reduces PGE2 levels in the cerebrospinal fluid in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse collagen-induced arthritis (CIA) model[1]
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Dosage:100 mg/kg
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Administration:PO, BID for 31 days
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Result:Gave a dramatic reduction in the clinical disease severity score relative to the vehicle treated group.
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Animal Model:Male Sprague-Dawley rats[2]
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Dosage:100 nM in 5 μL of 100% DMSO/rat
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Administration:Intrathecal administration
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Result:Reduced PGE2 levels in the cerebrospinal fluid (CSF) by 45-60%, yet there was no effect on the nociceptive response.
Chemical Information
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No. CAS 381683-94-9
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Peso molecular 746.14
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Fòrmula C40H35Cl3N2O4S
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SMILES
ClC1=C(Cl)C=CC(CS(NCCC2=C(CCCC3=CC=C(C(O)=O)C=C3)C4=CC(Cl)=CC=C4N2C(C5=CC=CC=C5)C6=CC=CC=C6)(=O)=O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[2]. Nickerson-Nutter CL, et al. The cPLA2α inhibitor efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid. Neuropharmacology. 2011 Mar;60(4):633-41. [Content Brief]
[3]. Niknami M, et al. Decrease in expression or activity of cytosolic phospholipase A2alpha increases cyclooxygenase-1 action: A cross-talk between key enzymes in arachidonic acid pathway in prostate cancer cells. Biochim Biophys Acta. 2010 Jul;1801(7):731-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Efipladib Related Classifications
HY-106253 Related Classifications
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