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首页-小分子抑制剂&激动剂-GPCR-Trace Amine-associated Receptor (TAAR)-RO 5166017
RO 5166017

Chemical Structure : RO 5166017

CAS No.: 1048346-74-2

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RO 5166017 (RO5166017;RO-5166017)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 219.288
    分子式 C12H17N3O
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (S)-4-[(ethyl-phenyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine

    参考文献

    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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