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GSK598809

Chemical Structure : GSK598809

CAS No.: 863680-45-9

GSK598809 (GSK 598809;GSK-598809)

Catalog No.: PC-60743Not For Human Use, Lab Use Only.

GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

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

    Biological Activity

    GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9; displays >100-fold selectivity over D2 and H1 receptors; significantly attenuates the expression of conditioned place preference (CPP) to nicotine and cocaine; potentiates the hemodynamic effects of cocaine in dogs, also increases mean arterial blood pressure and heart rate in vivo.

    Other Indication

    Phase 2 Clinical

    Physicochemical Properties

    M.Wt 481.514
    Formula C22H23F4N5OS
    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

    1-[2-Fluoro-4-(trifluoromethyl)phenyl]-3-[3-[[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio]propyl]-3-azabicyclo[3.1.0]hexane

    References

    1. Micheli F, et al. J Med Chem. 2010 Jan 14;53(1):374-91.

    2. Appel NM, et al. J Pharmacol Exp Ther. 2015 Sep;354(3):484-92.

    3. Dodds CM, et al. Appetite. 2012 Aug;59(1):27-33.

    4. Searle G, et al. Biol Psychiatry. 2010 Aug 15;68(4):392-9.

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