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Products Details
Product Description
– 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].
Web ID
– HY-106253
Shipping
– Room temperature
Applications
– COVID-19-immunoregulation
Molecular Formula
– C40H35Cl3N2O4S
References
– [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.
CAS Number
– 381683-94-9
Molecular Weight
– 746.14
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
Clinical Information
– No Development Reported
Research Area
– Inflammation/Immunology
Solubility
– 10 mM in DMSO
Target
– Phospholipase
Isoform
– Phospholipase A
Pathway
– Metabolic Enzyme/Protease
Product type
– Reference compound
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