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    Lumiracoxib (CGS 35189; COX 189)
    Lumiracoxib (CGS 35189; COX 189)

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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 #: V1068
    CAS #: 220991-20-8Purity ≥98%

    Description: Lumiracoxib (formerly CGS-35189; COX-189; trade name Prexige), a non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 enzyme inhibitor with potential anti-inflammatory activity. It inhibits COX-2 with an IC50 and a Ki of 0.14 μM and 0.06 μM, and exhibits 515-fold selectivity for COX-2 over COX-1. Lumiracoxib has anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety. Lumiracoxib has an IC50 of 0.14 μm in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 μm.

    References: Br J Pharmacol. 2005 Feb;144(4):538-50.

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    Molecular Weight (MW)293.72 
    FormulaC15H13ClFNO2 
    CAS No.220991-20-8 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 59 mg/mL (200.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)

    Chemical Name: 2-(2-((2-chloro-6-fluorophenyl)amino)-5-methylphenyl)acetic acid

    InChi Key: KHPKQFYUPIUARC-UHFFFAOYSA-N

    InChi Code: InChI=1S/C15H13ClFNO2/c1-9-5-6-13(10(7-9)8-14(19)20)18-15-11(16)3-2-4-12(15)17/h2-7,18H,8H2,1H3,(H,19,20)

    SMILES Code: O=C(O)CC1=CC(C)=CC=C1NC2=C(F)C=CC=C2Cl

    SynonymsLumiracoxib; COX-189; CGS-35189; CGS 35189; COX189; CGS35189; COX 189; trade name: Prexige.


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    In Vitro

    In vitro activity: Lumiracoxib has an IC50 of 0.14 μm in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 μm (HEK 293 cells transfected with human COX-1). In a human whole blood assay, IC50 values for Lumiracoxib are 0.13 μM for COX-2 and 67 μM for COX-1 (COX-1/COX-2 selectivity ratio 515).

    In VivoLumiracoxib is a highly selective COX-2 inhibitor with anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety. Lumiracoxib is rapidly absorbed following oral administration in rats with peak plasma levels being reached between 0.5 and 1 h. Efficacy of Lumiracoxib in rat models of hyperalgesia, oedema, pyresis and arthritis is dose-dependent and similar to diclofenac. However, consistent with its low COX-1 inhibitory activity, Lumiracoxib at a dose of 100 mg/kg orally causes no ulcers and is significantly less ulcerogenic than diclofenac.
    Animal modelFemale Lewis rats 
    Formulation & DosageDissolved in phosphate-buffered saline; 0.2–2 mg/kg; Oral gavage
    References

    Br J Pharmacol. 2005 Feb;144(4):538-50. 


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

    Lumiracoxib

    Inhibition of COX-1 and COX-2 in cell-based assays. Br J Pharmacol. 2005 Feb;144(4):538-50.
     

    Lumiracoxib

    In vitro inhibition of COX-1 and COX-2 in human blood assays. Br J Pharmacol. 2005 Feb;144(4):538-50.
     

    Lumiracoxib

    In vivo anti-inflammatory efficacy of lumiracoxib and diclofenac.



    Lumiracoxib

    Inhibition of ex vivo COX-1-dependent TxB2 and in vivo COX-2-dependent PGE2 in rat. Br J Pharmacol. 2005 Feb;144(4):538-50.


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