Nepafenac

Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM) . Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries[1][2][3].

Product Specifications

CAS Number

[78281-72-8]

Product Name Alternative

AHR 9434; AL 6515

UNSPSC

12352005

Hazard Statement

H400

Target

COX; Endogenous Metabolite; Prostaglandin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Endocrinology; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Nepafenac.html

Purity

99.56

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N)CC1=CC=CC(C(C2=CC=CC=C2)=O)=C1N

Molecular Formula

C15H14N2O2

Molecular Weight

254.28

Precautions

H400

References & Citations

[1]Gamache DA, Graff G, Brady MT et al. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000 Aug;24 (4) :357-70.|[2]Ke TL, Graff G, Spellman JM, Yanni JM. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: II. In vitro bioactivation and permeation of external ocular barriers. Inflammation. 2000 Aug;24 (4) :371-84.|[3]Marshall JC, Fernandes BF, Di Cesare S et al. The use of a cyclooxygenase-2 inhibitor (Nepafenac) in an ocular and metastatic animal model of uveal melanoma. Carcinogenesis. 2007 Sep;28 (9) :2053-8.