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    Nepafenac (AHR9434; AL6515; Nevanac)
    Nepafenac (AHR9434; AL6515; Nevanac)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1039
    CAS #: 78281-72-8Purity ≥98%

    Description: Nepafenac (formerly AHR9434; AL 6515; AL-6515; AHR-9434; Nevanac; Nevanac) is a potent non-steroidal anti-inflammatory drug (NSAID), and a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 enzyme activity. It was approved for the treatment of pain and inflammation associated with cataract surgery. 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.

    References: Inflammation. 2000 Aug;24(4):357-70; Inflammation. 2003 Oct;27(5):281-91; Invest Ophthalmol Vis Sci. 2003 Jan;44(1):409-15. 

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    Molecular Weight (MW)254.28
    FormulaC15H14N2O2
    CAS No.78281-72-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 50 mg/mL (196.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 2-(2-amino-3-benzoylphenyl)acetamide

    InChi Key: QEFAQIPZVLVERP-UHFFFAOYSA-N

    InChi Code: InChI=1S/C15H14N2O2/c16-13(18)9-11-7-4-8-12(14(11)17)15(19)10-5-2-1-3-6-10/h1-8H,9,17H2,(H2,16,18)

    SMILES Code: O=C(N)CC1=CC=CC(C(C2=CC=CC=C2)=O)=C1N

    SynonymsAHR 9434, AHR 9434; AHR9434; AL 6515; AL-6515; AHR-9434; Nevanac; Nepafenac; Nevanac


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    In Vitro

    In vitro activity: 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.


    Cell Assay: 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.

    In VivoNepafenac shows significantly greater ocular bioavailability and amfenac demonstrated greater potency at COX-2 inhibition than ketorolac or bromfenac. Nepafenac exhibits only weak COX-1 inhibitory activity with IC50 of 64.3 mM. Nepafenac inhibits prostaglandin synthesis in the iris/ciliary body (85-95%) and the retina/choroid (55%) in rabbits. Nepafenac (0.5%) produces 65% reduction in retinal edema which is correlated with 62% inhibition of blood-retinal barrier breakdown. Nepafenac (0.5%) significantly inhibits (46%) blood-retinal barrier breakdown concomitant with near total suppression of PGE2 synthesis (96%). Nepafenac significantly inhibits retinal prostaglandin E(2), superoxide, cyclooxygenase-2, and leukostasis within retinal microvessels in insulin-deficient diabetic rats, without affecting vascular endothelial growth factor (VEGF) and nitric oxide (NO). Nepafenac significantly inhibits the number of transferase-mediated dUTP nick-end labeling-positive capillary cells, acellular capillaries, and pericyte ghosts in diabetic rats. Nepafenac results in significantly less choroidal neovascularization and significant less ischemia-induced retinal neovascularization in mice compare to control. Nepafenac also blunts the increase in VEGF mRNA in the retina induced by ischemia. Nepafenac delays the progression of malignancy as well as reduces weight in an ocular and metastatic animal model of uveal melanoma.
    Animal modelNepafenac 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  
    Formulation & DosageN/A
    References

    Inflammation. 2000 Aug;24(4):357-70; Inflammation. 2003 Oct;27(5):281-91; Invest Ophthalmol Vis Sci. 2003 Jan;44(1):409-15. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Nepafenac

    Post-operative change in macular volume in patients without risk factors (95% CI). BMC Ophthalmol. 2017 Feb 20;17(1):16. 
     

    Nepafenac

    Post-operative change in macular volume in patients with risk factors (95% CI). BMC Ophthalmol. 2017 Feb 20;17(1):16. 


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