Nepafenac

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.
Targets
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]

Protocol

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
Formula

C15H14N2O2

CAS No. 78281-72-8
Storage powder
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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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COX Signaling Pathway Map

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