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Efipladib

CAS No. 381683-94-9

Efipladib( PLA 902 )

Catalog No. M14320 CAS No. 381683-94-9

Efipladib (PLA 902) is a potent, selective and orally active inhibitor of cPLA2α with IC50 of 20 nM for LTB4 inhibition.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Efipladib
  • Note
    Research use only, not for human use.
  • Brief Description
    Efipladib (PLA 902) is a potent, selective and orally active inhibitor of cPLA2α with IC50 of 20 nM for LTB4 inhibition.
  • Description
    Efipladib (PLA 902) is a potent, selective and orally active inhibitor of cPLA2α with IC50 of 20 nM for LTB4 inhibition; shows efficacy in multiple acute and chronic prostaglandin and leukotriene dependent in vivo models; also decreases basal and EGF-stimulated AKT phosphorylation and proliferation in HT-29 cancer cells, reduces xenograft growth by >90% with a concomitant decrease in AKT phosphorylation in mice (10 mg/kg, i.p. daily, >14 days).Rheumatoid Arthritis Phase 2 Discontinued.
  • In Vitro
    Western Blot Analysis Cell Line:PC3 and LNCaP cells Concentration:10, 15, 20 and 25 μM Incubation Time:72 h Result:Significantly decreased cPLA2α activity. Increased COX-1 protein levels. Increased COX-2 protein levels in PC3 cells.
  • In Vivo
    Animal Model:Mouse collagen-induced arthritis (CIA) model Dosage:100 mg/kg Administration:PO, BID for 31 daysResult:Gave a dramatic reduction in the clinical disease severity score relative to the vehicle treated group.Animal Model:Male Sprague-Dawley rats Dosage:100 nM in 5 μL of 100% DMSO/rat Administration:Intrathecal administration Result:Reduced PGE2 levels in the cerebrospinal fluid (CSF) by 45-60%, yet there was no effect on the nociceptive response.
  • Synonyms
    PLA 902
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    Phospholipase
  • Recptor
    Phospholipase
  • Research Area
    Inflammation/Immunology
  • Indication
    Rheumatoid Arthritis

Chemical Information

  • CAS Number
    381683-94-9
  • Formula Weight
    746.14
  • Molecular Formula
    C40H35Cl3N2O4S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C(O)C1=CC=C(CCCC2=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
  • Chemical Name
    4-(3-(5-chloro-2-(2-(((3,4-dichlorobenzyl)sulfonyl)aMino)ethyl)-1-(diphenylMethyl)-1H-indol-3-yl)propyl)benzoic acid

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. McKew JC, et al. J Med Chem. 2008 Jun 26;51(12):3388-413. 2. Nickerson-Nutter CL, et al. Neuropharmacology. 2011 Mar;60(4):633-41. 3. Zheng Z, et al. Oncotarget. 2014 Dec 15;5(23):12304-16.
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