Catalog No.S1255 Synonyms: AHR 9434, AL 6515

Nepafenac Chemical Structure

Molecular Weight(MW): 254.28

Nepafenac is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery.

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Biological Activity

Description Nepafenac is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery.
COX1 [1] COX2 [1]
In vivo Nepafenac shows significantly greater ocular bioavailability and amfenac demonstrated greater potency at COX-2 inhibition than ketorolac or bromfenac. [1] Nepafenac exhibits only weak COX-1 inhibitory activity with IC50 of 64.3 mM. Nepafenac inhibits prostaglandin synthesis in the iris/ciliary body (85-95%) and the retina/choroid (55%) in rabbits. [2] Nepafenac (0.5%) produces 65% reduction in retinal edema which is correlated with 62% inhibition of blood-retinal barrier breakdown. Nepafenac (0.5%) significantly inhibits (46%) blood-retinal barrier breakdown concomitant with near total suppression of PGE2 synthesis (96%). [3] Nepafenac significantly inhibits retinal prostaglandin E(2), superoxide, cyclooxygenase-2, and leukostasis within retinal microvessels in insulin-deficient diabetic rats, without affecting vascular endothelial growth factor (VEGF) and nitric oxide (NO). Nepafenac significantly inhibits the number of transferase-mediated dUTP nick-end labeling-positive capillary cells, acellular capillaries, and pericyte ghosts in diabetic rats. [4] Nepafenac results in significantly less choroidal neovascularization and significant less ischemia-induced retinal neovascularization in mice compare to control. Nepafenac also blunts the increase in VEGF mRNA in the retina induced by ischemia. [5] Nepafenac delays the progression of malignancy as well as reduces weight in an ocular and metastatic animal model of uveal melanoma. [6]


Solubility (25°C)

In vitro DMSO 50 mg/mL (196.63 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 254.28


CAS No. 78281-72-8
Storage powder
in solvent
Synonyms AHR 9434, AL 6515

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02955641 Not yet recruiting Glaucoma, Closed-Angle|Glaucoma, Narrow-Angle|Glaucoma, Angle-Closure Sheba Medical Center November 2016 --
NCT02821390 Active, not recruiting Pain University Hospital of Patras June 2016 --
NCT02752646 Recruiting Cataract MDbackline, LLC|Alcon Research April 2016 --
NCT01939691 Not yet recruiting Uveitis|Cystoid Macular Edema University of California, San Francisco December 2015 Phase 4
NCT02506348 Recruiting Post Surgical Management|Pain Management|Inflamation Management Wolfson Medical Center July 2015 --
NCT02361645 Completed Vitreous Inflammation Università degli Studi di Brescia March 2014 Phase 3

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID