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: 78281-72-8

Selleck's Nepafenac has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.95%
99.95

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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.
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 lnformation & 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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