Cart
sales@molnova.com
Home - Products - Metabolic Enzyme/Protease - Phospholipase - Efipladib

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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 1143 Get Quote
50MG 2322 Get Quote
100MG 3060 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote
Get Quotation Bulk Inquiry Add to Cart

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.
Calculator

Molecular Weight Calculator

Dilution Calculator

Molarity Calculator

molnova catalog
related products

  • Abbolactone

    Spironolactone is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.

  • VU0155069

    VU0155069 strongly inhibits the invasive migration of several cancer cell lines in transwell assays. VU0155069 is a selective phospholipase D1 inhibitor (IC50: 46 nM in vitro).

  • Atg4B-IN-2

    Atg4B-IN-2. A potent, selective Atg4B inhibitor with anticancer activity, inhibits both Atg4B and PLA2, enabling autophagy that counteracts the anticancer activity of anti-desiccation-resistant prostate cancer drugs.

Sign In Join Free