Nepafenac

Short Summary : COX-1 and COX-2 inhibitor

Category : Neuroscience|COX

Purity : 0.98

CAS Number : 78281-72-8

Formula : C15H14N2O2

Molecular Weight : 254.28

SMILE : C1=CC=C(C=C1)C(=O)C2=C(C(=CC=C2)CC(=O)N)N

Solubility : >10mg/mL in DMSO

Storage : Store at -20°C

Description : Nepafenac is a non-steroidal anti-inflammatory drug (NSAID). The IC50 values of nepafenac for (cyclooxygenase-1) COX-1 and COX-2 are 250 nM and 150 nM, respectively [1].Nepafenac showed to significantly decrease the retinal levels of PGE2 in LPS-induced rats when administrated topically. However, nepafenac has revealed no significant effect on BRB permeability in LPS-induced rat model [1].Nepafenac significantly reduced proliferation rate of human uveal melanoma cell lines including SP6.5, 92.1, OCM-1, MKT-BR and of human transformed uveal melanocyte cell line UW-1. Compared to rofecoxib, nepafenac might reveal a better systemic safety profile [2].References:[1] Bucolo C1, Marrazzo G, Platania CB, Romano GL, Drago F, Salomone S. Effects of topical indomethacin, bromfenac and nepafenac on lipopolysaccharide-induced ocular inflammation. J Pharm Pharmacol. 2014 Jul;66(7):954-60. [2] Marshall JC1, Caissie AL, Cruess SR, Cools-Lartigue J, Burnier MN Jr. The effects of a cyclooxygenase-2 (COX-2) expression and inhibition on human uveal melanoma cell proliferation and macrophage nitric oxide production. J Carcinog. 2007 Nov 27;6:17.

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