Home Neuronal Signaling COX inhibitor Nepafenac For research use only.

Nepafenac

Synonyms: AHR 9434, AL 6515

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.

Nepafenac Chemical Structure

Nepafenac Chemical Structure

CAS No. 78281-72-8

Purity & Quality Control

Nepafenac Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

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.
Targets
COX1 [1] COX2 [1]
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02821390 Completed
Pain
University Hospital of Patras
 June 2016 Not Applicable
NCT02752646 Completed
Cataract
MDbackline LLC|Alcon Research
 April 2016 Not Applicable

Chemical Information & Solubility

Molecular Weight 254.28 Formula

C15H14N2O2
CAS No. 78281-72-8 SDF Download Nepafenac SDF
Smiles C1=CC=C(C=C1)C(=O)C2=CC=CC(=C2N)CC(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 51 mg/mL ( (200.56 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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