For research use only.

Catalog No.S1255 Synonyms: AHR 9434, AL 6515

1 publication

Nepafenac Chemical Structure

CAS No. 78281-72-8

Nepafenac (AHR 9434, AL 6515) 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.

Selleck's Nepafenac has been cited by 1 publication

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Biological Activity

Description Nepafenac (AHR 9434, AL 6515) 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

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Chemical Information

Molecular Weight 254.28


CAS No. 78281-72-8
Storage powder
in solvent
Synonyms AHR 9434, AL 6515
Smiles C1=CC=C(C=C1)C(=O)C2=CC=CC(=C2N)CC(=O)N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02821390 Completed Drug: Nepafenac Eye Drops|Drug: Placebo (Artificial Tears) Pain University Hospital of Patras June 2016 Not Applicable
NCT02752646 Completed Drug: nepafenac 0.3%|Drug: ketorolac Cataract MDbackline LLC|Alcon Research April 2016 Not Applicable

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID