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    BMS-538203
    BMS-538203

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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 #: V2865
    CAS #: 543730-41-2Purity ≥98%

    Description: BMS-538203 is a novel and highly efficient HIV integrase inhibitor that is being developed as an antiviral agent. BMS-538203 was discovered by a hit-to-clinical candidate pathway that resulted in 50- and 2000-fold improvements in enzyme-inhibition and antiviral activity without an increase in molecular weight or change in molecular topology. The original hit, 1 (mw = 268) was optimized in a stepwise manner. Potential covalent protein-binding moieties were removed by reducing the number of the ketone groups. High enzyme inhibition activity was achieved by optimizing the aryl-portion of the molecule. Protein binding was reduced by replacing the standard amide by the corresponding methyl-hydroxamide. This eventually led to the discovery of compound 2 (BMS-538203, mw = 269) a highly efficient inhibitor and antiviral agent. 

    References: RU patent 2367439.

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    Molecular Weight (MW)269.23
    FormulaC12H12FNO5 
    CAS No.543730-41-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: ≥ 54 mg/mL
    Water:<1 mg/mL 
    Ethanol:<1 mg/mL
    SMILES CodeO=C(O)/C(O)=C/C(N(CC1=CC=C(F)C=C1)OC)=O
    SynonymsBMS-538203; BMS538203; BMS 538203.


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    In Vitro

    In vitro activity: BMS-538203 is a novel and highly efficient HIV integrase inhibitor and antiviral agent. BMS-538203 was discovered by a hit-to-clinical candidate pathway that resulted in 50- and 2000-fold improvements in enzyme-inhibition and antiviral activity without an increase in molecular weight or change in molecular topology. The original hit, 1 (mw = 268) was optimized in a stepwise manner. Potential covalent protein-binding moieties were removed by reducing the number of the ketone groups. High enzyme inhibition activity was achieved by optimizing the aryl-portion of the molecule. Protein binding was reduced by replacing the standard amide by the corresponding methyl-hydroxamide. This eventually led to the discovery of compound 2 (BMS-538203, mw = 269) a highly efficient inhibitor and antiviral agent. 

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    Formulation & Dosage
    ReferencesRU patent 2367439.


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

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