Efipladib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Efipladib (PLA 902) 是一种有效的、选择性的、口服活性的 cPLA2α 抑制剂，抑制 LTB4 的 IC50 为 20 nM。

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.

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.

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.

PLA 902

Metabolic Enzyme/Protease

Phospholipase

Phospholipase

Inflammation/Immunology

Rheumatoid Arthritis

381683-94-9

746.14

C40H35Cl3N2O4S

>98% (HPLC)

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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

4-(3-(5-chloro-2-(2-(((3,4-dichlorobenzyl)sulfonyl)aMino)ethyl)-1-(diphenylMethyl)-1H-indol-3-yl)propyl)benzoic acid

(-20℃)

With Ice Pack

≥ 2 years