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GZ-11608

Chemical Structure : GZ-11608

CAS No.: 2141974-01-6

GZ-11608 (GZ11608)

Catalog No.: PC-47107Not For Human Use, Lab Use Only.

GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with Ki of 25 nM, GZ-11608 (EC50=620 nM) released vesicular dopamine 25-fold less potently than it inhibited VMAT2 dopamine uptake.

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

    Biological Activity

    GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with Ki of 25 nM, GZ-11608 (EC50=620 nM) released vesicular dopamine 25-fold less potently than it inhibited VMAT2 dopamine uptake.
    GZ-11608 displays selectivity (92-1180-fold) for VMAT2 over nicotinic receptors, dopamine transporter, and hERG, suggesting low side-effects.
    GZ-11608 competitively inhibited methamphetamine-evoked vesicular dopamine release.
    GZ-11608 decreased methamphetamine sensitization without altering striatal dopamine content or exacerbating methamphetamine-induced dopamine depletion, revealing efficacy without neurotoxicity.
    GZ-11608 exhibited linear pharmacokinetics and rapid brain penetration.
    GZ-11608 decreased methamphetamine self-administration in drug-naive rats.

    Physicochemical Properties

    M.Wt 283.415
    Formula C19H25NO
    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

    S-3-(4-methoxyphenyl)-N-(1-phenylpropan-2-yl)propan-1-amine

    References

    1. Lee NR, et al. J Pharmacol Exp Ther. 2019 Nov;371(2):526-543.

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