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[1].

Product Specifications

CAS Number

[381683-94-9]

UNSPSC

12352005

Target

Phospholipase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/efipladib.html

Solubility

10 mM in DMSO

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

Molecular Formula

C40H35Cl3N2O4S

Molecular Weight

746.14

References & Citations

[1]McKew J C, et al. Indole Cytosolic Phospholipase A2 α Inhibitors: Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2- (2-{[ (3, 4-dichlorobenzyl) sulfonyl] amino} ethyl) -1- (diphenylmethyl) -1 H-indol-3-yl] propyl} benzoic Acid, Efipladib. Journal of medicinal chemistry, 2008, 51 (12) : 3388-3413.|[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.|[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.