| Identification | Back Directory | [Name]
EFIPLADIB | [CAS]
381683-94-9 | [Synonyms]
PLA902
PLA-902
PLA 902
EFIPLADIB
Efipladib
(PLA 902)
4-(3-(1-benzhydryl-5-chloro-2-(2-((3,4-dichlorophenyl)MethylsulfonaMido)ethyl)-1H-indol-3-yl)propyl)benzoic acid
4-(3-(5-chloro-2-(2-(((3,4-dichlorobenzyl)sulfonyl)aMino)ethyl)-1-(diphenylMethyl)-1H-indol-3-yl)propyl)benzoic acid
Benzoic acid, 4-[3-[5-chloro-2-[2-[[[(3,4-dichlorophenyl)methyl]sulfonyl]amino]ethyl]-1-(diphenylmethyl)-1H-indol-3-yl]propyl]- | [Molecular Formula]
C40H35Cl3N2O4S | [MDL Number]
MFCD09833236 | [MOL File]
381683-94-9.mol | [Molecular Weight]
746.14 |
| Hazard Information | Back Directory | [Uses]
Treatment of pain and symptomatic management of arthritis. | [in vivo]
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]. | Animal Model: | Mouse collagen-induced arthritis (CIA) model[1] | | Dosage: | 100 mg/kg | | Administration: | PO, BID for 31 days | | Result: | Gave a dramatic reduction in the clinical disease severity score relative to the vehicle treated group. |
| Animal Model: | Male Sprague-Dawley rats[2] | | 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. |
| [IC 50]
cPLA2α: 0.04 μM (IC50); cPLA2α: 0.067 μM (Ki) |
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