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GTPL3347, SCHEMBL143540

A Potent Antagonist of mGluR1 Receptors

Cat #: L-240
Alternative Name GTPL3347, SCHEMBL143540
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 341.47
    Purity: >99%
    Effective concentration 1 nM – 1 µM.
    Chemical name 2-[[4-(2,3-dihydro-1H-inden-2-ylamino)-5,6,7,8-tetrahydroquinazolin-2-yl]sulfanyl]ethanol.
    Molecular formula C19H23N3OS.
    PubChem CID 9840951
    Activity LY456066 is a potent antagonist of mGluR1 receptors. It inhibits human mGluR1 receptors expressed in CHO cells with an IC50 of 28 nM1.
    1. Fukuda, J. et al. (2009) Neuropharmacology 57, 438.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs LY456066 inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs LY456066 inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Dose-response of normalized inhibition of human mGluR1 mediated, L-Glutamate evoked Ca2+ mobilization by LY456066 (#L-240). IC50 was determined at 14.9 nM. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with a range of concentrations of LY456066, and stimulated by 15 µM L-Glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    1. Fukuda. J. et al. (2009) Neuropharmacology 57, 438.
    2. Suzuki, G. et al. (2007) J. Pharmacol. Exp. Ther. 321, 1144.
    3. Tsui, H.T. et al. (2002) Soc. Neurosci. Meet. Abstract No. 247.3.
    4. Eom, H.S. et al. (2016) PLoS One 11, e0147538.
    Scientific background

    LY456066 is a selective, negative allosteric modulator of mGluR1 receptors. The compound demonstrates high potent antagonistic activities toward both rat and human mGluR1 receptor with an IC50 value of 28 nM for human mGluR1 receptors expressed in Chinese hamster ovary cells1,2. Several studies have suggested that LY456066 may bind to a site at the mGluR1 receptor that could represent a conserved negative allosteric regulatory domain3.

    Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) that play an important role in synaptic plasticity and other neurophysiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly found on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cell and the formation of the hippocampus4.

    Target mGluR1
    Last update: 02/01/2022

    LY456066 (#L-240) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background

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