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Nepafenac

CAT: 0804-HY-17357-01Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-17357-01Size:25 mg
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Description
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 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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
COX-1; COX-2

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