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    Amfenac Sodium Monohydrate
    Amfenac Sodium Monohydrate

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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 #: V1075
    CAS #: 61618-27-7Purity ≥98%

    Description: Amfenac Sodium monohydrate (AHR 5850; AHR5850; AHR5850), the sodium salt of amfenac which is an NSAID, is a non-steroidal analgesic anti-inflammatory agent with antipyretic and analgesic activities. It acts as an inhibitor of COX-1 and COX-2 enzymes with IC50s of 15.3 and 20.4 nM, respectively. Amfenac is transformed in vivo to the active metabolite nepafenac which is also  a non-steroidal anti-inflammatory drug (NSAID). 

    References: Inflammation. 2000 Aug;24(4):357-70; Agents Actions. 1977 Mar;7(1):133-44.

    Related CAS#: 61941-56-8 (sodium); 51579-82-9 (free acid); 61618-27-7 (Sodium Monohydrate)

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    Molecular Weight (MW)295.27 
    FormulaC15H12NO3.H2O.Na 
    CAS No.61618-27-7  
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 59 mg/mL (199.8 mM) 
    Water: 59 mg/mL (199.8 mM) 
    Ethanol: 4 mg/mL (13.5 mM) 
    Other infoChemical Name: Benzeneacetic acid, 2-amino-3-benzoyl-, sodium salt, monohydrate

    InChi Key: QZNJPJDUBTYMRS-UHFFFAOYSA-M

    InChi Code: InChI=1S/C15H13NO3.Na.H2O/c16-14-11(9-13(17)18)7-4-8-12(14)15(19)10-5-2-1-3-6-10;;/h1-8H,9,16H2,(H,17,18);;1H2/q;+1;/p-1

    SMILES Code: O=C([O-])CC1=CC=CC(C(C2=CC=CC=C2)=O)=C1N.[H]O[H].[Na+]           

    SynonymsAHR 5850; AHR5850; AHR5850


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    In Vitro

    In vitro activity: Amfenac is a potent inhibitor of both COX-1 and COX-2 with IC50 of 0.25 and 0.15 μM.


    Cell Assay: Human uveal melanoma cell lines are transfected to constitutively express COX-2 and the proliferative rate of these cells using two different methods, with and without the addition of Amfenac Sodium Hydrate, is measured. Nitric oxide production by macrophages is measured after exposure to melanoma-conditioned medium from both groups of cells as well as with and without Amfenac Sodium Hydrate

    In VivoAmfenac possesses both antipyretic and analgesic properties in vivo. Amfenac (4 mg/kg) suppressed acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation by 33% and 28%, respectively, which is 16.4 and 22.8 times more potent than phenylbutazone. The analgesic activity of Amfenac is 43 times that of acetylsalicylic acid in the Randall-Selitto assay, and 156 and 56.3 times more potent than phenylbutazone in the acetylcholine-induced abdominal constriction in mice and in the bradykinin-induced nociceptive response in dogs, respectively. Amfenac produces less gastric irritation than acetylsalicylic acid when applied topically to the exposed gastric mucosa of cats or when administered orally to rats and dogs. Upon subchronic oral administration to rats, the therapeutic ratio of Amfenac is twice that of phenylbutazone. 
    Animal modelCats, rats, dogs
    Formulation & Dosagetopical
    References

    Inflammation. 2000 Aug;24(4):357-70; Agents Actions. 1977 Mar;7(1):133-44; J Carcinog. 2007 Nov 27;6:17.


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

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