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RTI-7470-44

Chemical Structure : RTI-7470-44

CAS No.: 825658-63-7

RTI-7470-44 (TAAR1 antagonist)

Catalog No.: PC-72353Not For Human Use, Lab Use Only.

RTI-7470-44 is a potent, selective human trace amine-associated receptor subtype 1 (hTAAR1) inhibitor with IC50 of 8.4 nM in vitro cAMP functional assay.

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

    Biological Activity

    RTI-7470-44 is a potent, selective human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with IC50 of 8.4 nM in vitro cAMP functional assay.
    RTI-7470-44 exhibits a Ki of 0.3 nM in a radioligand binding assay, and shows species selectivity (>90-fold) for hTAAR1 over the rat and mouse orthologues.
    RTI-7470-44 displays good blood–brain barrier permeability, moderate metabolic stability, and a favorable preliminary off-target profile.
    RTI-7470-44 increased the spontaneous firing rate of mouse VTA dopaminergic neurons and blocked the effects of the known TAAR1 agonist RO5166017.

    Physicochemical Properties

    M.Wt 449.836
    Formula C19H11ClF3N5OS
    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

    2-((6-(4-chlorophenyl)-3-cyano-4-(trifluoromethyl)pyridin-2-yl)thio)-N-(pyrimidin-2-yl)acetamide

    References

    1. Ann M Decker, et al. ACS Chem Neurosci. 2022 Mar 24. doi: 10.1021/acschemneuro.2c00086.

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