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MK-4256

Chemical Structure : MK-4256

CAS No.: 1104599-69-0

MK-4256 (MK 4256;MK4256)

Catalog No.: PC-61088Not For Human Use, Lab Use Only.

MK-4256 is a potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    MK-4256 is a potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5.
    MK-4256 reduces glucose excursion in a dose-dependent fashion with maximal efficacy achieved at doses as low as 0.03 mg/kg po, with minimal hypoglycemia risk.
    Preclinical tirals of MK-4256 are discontinued due to dose-dependent QTc in conscious cardiovascular (CV) dog model.

    Physicochemical Properties

    M.Wt 494.534
    Formula C27H23FN8O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    3-((1R,3R)-3-(5-(4-fluorophenyl)-1H-imidazol-2-yl)-1-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)-5-methyl-1,2,4-oxadiazole

    References

    1. He S, et al. ACS Med Chem Lett. 2012 May 7;3(6):484-9.

    2. He S, et al. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53.

    3. He S, et al. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1529-1535.

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