2. Immunology/Inflammation GPCR/G Protein Metabolic Enzyme/Protease
  3. COX Prostaglandin Receptor Endogenous Metabolite
  4. Nepafenac

Nepafenac  (Synonyms: AHR 9434; AL 6515)

Cat. No.: HY-17357 Purity: 99.56%
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Handling Instructions Technical Support

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.

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Nepafenac

Nepafenac Chemical Structure

CAS No. : 78281-72-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Nepafenac:

Nepafenac Related Antibodies

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COX COX-1 COX-2 COX-3

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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 (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].

IC50 & Target[1]

COX-1

64.3 μM (IC50)

COX-2

0.12 μM (IC50)

In Vitro

Nepafenac (0.05%-0.1% eye drops, 0-500 min) inhibits PGE₂ 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 (kps) 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.

Nepafenac Related Antibodies
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
Molecular Weight

254.28

Formula

C15H14N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9327 mL 19.6634 mL 39.3267 mL
5 mM 0.7865 mL 3.9327 mL 7.8653 mL
View the Complete Stock Solution Preparation Table

* 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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.56%

SDS (398 KB)

COA (246 KB) HNMR (138 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Nepafenac Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nepafenac78281-72-8AHR 9434 AL 6515AHR9434AHR-9434AL6515AL 6515AL-6515COXProstaglandin ReceptorEndogenous MetaboliteCyclooxygenaseCMCcirculating malignant cellCOX-2cyclooxygenase-2CsAcyclosporin APCRpolymerase chain reactionUMuveal melanoma.Inhibitorinhibitorinhibit

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