Cat. No.: HY-17357

Nepafenac

(Synonyms: AHR 9434; AL 6515)

Customer Review

Based on 1 Customer Validation

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 PGE_₂. 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.

For research use only. We do not sell to patients.

Purity: 99.56%
CAS No.: 78281-72-8
Formula: C₁₅H₁₄N₂O₂
Molecular Weight:254.28

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nepafenac Chemical Structure

CAS No.: 78281-72-8

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

COX-1

64.3 μM (IC₅₀)

COX-2

0.12 μM (IC₅₀)

All COX Isoforms :

All Prostaglandin Receptor Isoforms :

In Vitro

Nepafenac (0.05%-0.1% eye drops, 0-500 min) inhibits PGE_₂ by 90-95% in the isolated rabbit iris/ciliary body and by 55% in the retina/choroid, for a duration of 6 hours and 4 hours, respectively at 1%^[1].
Nepafenac (7-117 μM, 0-400 min) has a stronger isolated rabbit corneal and conjunctiva/sclera permeability than Diclofenac (HY-15036) with permeation coefficients (k_ps) of 727 × 10^-6 min^-1 and 128 × 10^-6 min^-1, respectively^[2].
Nepafenac (0.05%-0.1% eye drops, 5 min) results in sustained flux of drug across the cornea for 6 h with short term perfusion of the isolated rabbit corneal surface and accumulates at 16.7 μM on the corneal endothelial side^[2].
Nepafenac (8.9-140 μM, 0-6 h) can effectively hydrolyze into Amfenac in the cornea, iris/ciliary body, and retina/choroid of both rabbit and human eyes, moreover, the hydrolysis in rabbit cornea shows time and dose dependence^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nepafenac (0.1% eye drops, topical ocular administration, single dose) demonstrates a powerful and long-lasting anti-inflammatory effect in a trauma-induced rabbit model of acute ocular inflammation^[1].
Nepafenac (0.3% eye drops, topical ocular administration, twice daily for 12 weeks) delays the progression of uveal melanoma (UM) in rabbits^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Trauma-induced model of acute ocular inflammation established in New Zealand Albino rabbits (2-2.5 kg)^[1]
Dosage:

0.1% eye drops
Administration:

Topical ocular administration, single dose
Result:

Reduced protein exudation by 61% and inhibited PGE₂ by 98%.
Exhibited the anti-inflammatory effect lasts for 8 hours after a single administration.

Animal Model:

Human UM cell line induced xenograft tumor model established in male New Zealand albino rabbits^[3]
Dosage:

0.3% eye drops
Administration:

Topical ocular administration, twice daily for 12 weeks
Result:

Reduced the incidence of tumors.
Alleviated the tumor morphology, mainly presenting as flat lesions (in the control group, large tumors accompanied by vitreous hemorrhage were more common).
Significantly reduced the staining intensity of COX-2 in tumors. Delayed the appearance time of circulating tumor cells (CMCs), and reduced the lung and liver metastasis of the tumor.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 78281-72-8
Appearance Solid
Molecular Weight 254.28
Formula C₁₅H₁₄N₂O₂
Color Light yellow to yellow
SMILES

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

AHR 9434; AL 6515
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (393.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.9327 mL

19.6634 mL

39.3267 mL

5 mM

0.7865 mL

3.9327 mL

7.8653 mL

10 mM

0.3933 mL

1.9663 mL

3.9327 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (398 KB)
- English - EN (398 KB)
- Français - FR (398 KB)
- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Portuguese - PT (398 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.9327 mL	19.6634 mL	39.3267 mL	98.3168 mL
	5 mM	0.7865 mL	3.9327 mL	7.8653 mL	19.6634 mL
	10 mM	0.3933 mL	1.9663 mL	3.9327 mL	9.8317 mL
	15 mM	0.2622 mL	1.3109 mL	2.6218 mL	6.5545 mL
	20 mM	0.1966 mL	0.9832 mL	1.9663 mL	4.9158 mL
	25 mM	0.1573 mL	0.7865 mL	1.5731 mL	3.9327 mL
	30 mM	0.1311 mL	0.6554 mL	1.3109 mL	3.2772 mL
	40 mM	0.0983 mL	0.4916 mL	0.9832 mL	2.4579 mL
	50 mM	0.0787 mL	0.3933 mL	0.7865 mL	1.9663 mL
	60 mM	0.0655 mL	0.3277 mL	0.6554 mL	1.6386 mL
	80 mM	0.0492 mL	0.2458 mL	0.4916 mL	1.2290 mL
	100 mM	0.0393 mL	0.1966 mL	0.3933 mL	0.9832 mL

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Nepafenac

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Endocrinology Compound Library

Anti-COVID-19 Compound Library

Pyroptosis Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Mechanoreceptors Compound Library

Anti-Colorectal Cancer Compound Library

Pediatric Drug Library

Antidepressant Compound Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Natural Product Diversity Scaffold Library

Lactylation Compound Library

All COX Isoforms

All Prostaglandin Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Nepafenac Related Classifications

Cat. No.: HY-17357