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Nepafenac (Synonyms: AHR 9434, AL 6515)

Catalog No.GC13637 Copy One-Click Copy Product Info

COX-1 and COX-2 inhibitor

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Nepafenac Chemical Structure

Cas No.: 78281-72-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$28.00
In stock
25mg
$25.00
In stock
100mg
$67.00
In stock

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Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.



Description of Nepafenac

Nepafenac is a non-steroidal anti-inflammatory drug (NSAID). The IC50 values of nepafenac for (cyclooxygenase-1) COX-1 and COX-2 are 250 nM and 150 nM, respectively [1].

Nepafenac showed to significantly decrease the retinal levels of PGE2 in LPS-induced rats when administrated topically. However, nepafenac has revealed no significant effect on BRB permeability in LPS-induced rat model [1].

Nepafenac significantly reduced proliferation rate of human uveal melanoma cell lines including SP6.5, 92.1, OCM-1, MKT-BR and of human transformed uveal melanocyte cell line UW-1. Compared to rofecoxib, nepafenac might reveal a better systemic safety profile [2].

References:
[1] Bucolo C1, Marrazzo G, Platania CB, Romano GL, Drago F, Salomone S. Effects of topical indomethacin, bromfenac and nepafenac on lipopolysaccharide-induced ocular inflammation. J Pharm Pharmacol. 2014 Jul;66(7):954-60.
[2] Marshall JC1, Caissie AL, Cruess SR, Cools-Lartigue J, Burnier MN Jr. The effects of a cyclooxygenase-2 (COX-2) expression and inhibition on human uveal melanoma cell proliferation and macrophage nitric oxide production. J Carcinog. 2007 Nov 27;6:17.

Chemical Properties of Nepafenac

Cas No. 78281-72-8 SDF
Synonyms AHR 9434, AL 6515
Chemical Name 2-(2-amino-3-benzoylphenyl)acetamide
Canonical SMILES C1=CC=C(C=C1)C(=O)C2=C(C(=CC=C2)CC(=O)N)N
Formula C15H14N2O2 M.Wt 254.28
Solubility ≥ 9.95mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Nepafenac

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.9327 mL 19.6634 mL 39.3267 mL
5 mM 786.5 μL 3.9327 mL 7.8653 mL
10 mM 393.3 μL 1.9663 mL 3.9327 mL
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In vivo Formulation Calculator (Clear solution) of Nepafenac

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Reviews

Review for Nepafenac

Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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