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    IEM 1754 2HBr
    IEM 1754 2HBr

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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 #: V1088
    CAS #: 162831-31-4Purity ≥98%

    Description: IEM 1754 2HBr (IEM-1754; IEM 1754; IEM1754), the dihydrobromide salt of IEM-1754, is a selective voltage-dependent open-channel blocker of AMPA/kainate receptors with important biological activity. It blocks GluR1 and GluR3 with an IC50 of 6 μM. 

    References: J Physiol. 1997 Dec 15;505 ( Pt 3):655-63; Br J Pharmacol. 2000 Jan;129(2):265-74.

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    Molecular Weight (MW)412.25
    FormulaC16H30N2.2HBr
    CAS No.162831-31-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 82 mg/mL (198.9 mM)
    Water: 82 mg/mL (198.9 mM) 
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    SynonymsIEM-1754;  IEM-1754 dihydrobromide; IEM 1754; IEM1754; IEM1754 dihydrobromide; IEM-1754 2HBr; IEM 1754 dihydrobromide; IEM 1754 2HBr; IEM1754 2HBr


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    In Vitro

    In vitro activity: IEM 1754 is an adamantane derivative. IEM 1754 causes use- and voltage-dependent block of open channels of recombinant AMPA receptors. This antagonism is dependent on receptor subunit composition, channels gated by recombinant, homomeric GluR1 and GluR3 receptors exhibites a higher sensitivity to block than those gated by receptors containing edited GluR2 subunits. IEM-1754 block of GluR2-containing AMPAR is enhanced by hyperpolarization in agreement with the classical single-exponential model. In contrast, the block of GluR2-lacking AMPAR is reduced by hyperpolarization

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    References

    J Physiol. 1997 Dec 15;505 ( Pt 3):655-63; Br J Pharmacol. 2000 Jan;129(2):265-74.


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

    IEM 1754 2HBr

    Voltage-dependence of IEM-1460 block. Br J Pharmacol. 2000 Jan;129(2):265-74.



    IEM 1754 2HBr

    Concentration-dependence of IEM-1460 block. Br J Pharmacol. 2000 Jan;129(2):265-74.

    IEM 1754 2HBr

    Voltage-dependence of equilibrium dissociation constant and kinetic rate constants for IEM-1460 block. Br J Pharmacol. 2000 Jan;129(2):265-74.
     

    IEM 1754 2HBr

    Proposed energy profiles for IEM-1460 block.



    IEM 1754 2HBr

    Comparison of the blocking effects of three dicationic compounds. Br J Pharmacol. 2000 Jan;129(2):265-74.


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