Efipladib 

Efipladib is a potent, selective and orally active cPLA₂α inhibitor with an IC₅₀ of 0.04 μM and a K_d of 0.067 μM^[1].

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.

Efipladib (100 mg/kg; p.o.; BID for 31 days) reverses the severity in mouse collagen-induced arthritis (CIA) model^[1].
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.

746.14

C₄₀H₃₅Cl₃N₂O₄S

381683-94-9

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [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]