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RO 5166017

Chemical Structure : RO 5166017

CAS No.: 1048346-74-2

RO 5166017 (RO5166017;RO-5166017)

Catalog No.: PC-61075Not For Human Use, Lab Use Only.

RO 5166017 is a potent, selective TAAR1 agonist with Ki of 1.9, 2.7, 31 and 24 nM for mouse, rat, cynomolgus monkey and human TAAR1 stably expressed in HEK293 cells.

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    Biological Activity

    RO 5166017 is a potent, selective TAAR1 agonist with Ki of 1.9, 2.7, 31 and 24 nM for mouse, rat, cynomolgus monkey and human TAAR1 stably expressed in HEK293 cells.
    RO 5166017 does not elicit cAMP production from mouse TAAR4 at 30 uM, and 79-, 64-, and 15-fold selectivity over κ-opioid, adrenergic α2, and imidazoline I1 receptors.
    RO 5166017 selectively inhibits the firing frequency of dopaminergic and serotonergic neurons in TAAR1 expressed regions in mouse brain slices (IC50=1.73 nM).
    RO 5166017 prevents stress-induced hyperthermia and blocks dopamine-dependent hyperlocomotion in cocaine-treated and dopamine transporter knockout mice.

    Physicochemical Properties

    M.Wt 219.288
    Formula C12H17N3O
    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)-4-[(ethyl-phenyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine

    References

    1. Revel FG, et al. Proc Natl Acad Sci U S A. 2011 May 17;108(20):8485-90.

    2. Revel FG, et al. Mol Psychiatry. 2013 May;18(5):543-56.

    3. Espinoza S, et al. Neuropsychopharmacology. 2015 Aug;40(9):2217-27.

    4. Alvarsson A, et al. J Neurosci. 2015 Oct 14;35(41):14057-69.

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