ML-301

ML301
A Selective Agonist of Neurotensin Receptor 1
  • New
Cat #: M-315
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 522.99
    Purity: >98%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name (2S)-2-[[1-(7-chloroquinolin-4-yl)-2-(2,6-dimethoxyphenyl)imidazole-4-carbonyl]amino]-4-methylpentanoic acid.
    Molecular formula C27H27ClN4O5.
    Activity ML-301 is a selective agonist of NTR1 receptors, shown to stimulate NTR1-mediated calcium mobilization with EC50 of 289 nM1-2.
    References - Activity
    1. Hershberger, P.M. et al. (2014) Bioorg. Med. Chem. Lett. 24, 262.
    2. Di Fruscia, P. et al. (2014) Bioorg. Med. Chem. Lett. 24, 3974.
    Storage before reconstitution 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.
    Reconstitution Soluble in DMSO.
    Centrifuge all products before handling (10000 x g 5 min).
    Storage after reconstitution Store at -20°C.
    It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    Alomone Labs ML-301 activates human NTR1 receptors expressed in CHO-K1 cells.
    Dose-response curve of hNTSR1 activation by ML-301 (#M-315), normalized to maximum effect of neurotensin. Cells were loaded with Fluo-8 dye and stimulated with increasing concentrations of ML-301. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence using FLIPRTETRA™.
    References - Scientific Background
    1. Hershberger, P.M. et al. (2014) Bioorg. Med. Chem. Lett. 24, 262.
    2. Di Fruscia, P. et al. (2014) Bioorg. Med. Chem. Lett. 24, 3974.
    Scientific background

    ML-301 is a fully selective imidazole-based agonist of neurotensin receptor 1 (NTR1). It stimulates NTR1-mediated calcium mobilization with an EC50 value of 289 nM1. The carboxylic acid moiety increases the compound’s solubility1.

    To date, four neurotensin receptors have been cloned from human: NTR1, NTR2, NTR3 and NTR4 which belong to the super family of G-protein coupled receptors (GPCRs). NTR1 mediates most of the known neurotensin ligand effects and is a potential therapeutic target2.

    Target Neurotensin Receptor 1

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    Last update: 22/11/2018

    ML-301 (#M-315) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Citations
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