SR 48692

SR48692, Meclinertant, Reminertant
A Potent and Selective Antagonist of Neurotensin Receptor 1
  • New
Cat #: S-265
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 587.07
    Purity: >98%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name 2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid.
    Molecular formula C32H31ClN4O5.
    CAS No.: 146362-70-1.
    Activity SR 48692 is a potent and selective non-peptide antagonist of NTS1 receptors, shown to inhibit neurotensin-stimulated IP production (Ki = 2.45 nM) and NTR1-mediated calcium mobilization1-3.
    References - Activity
    1. Labbe-Jullie, C. et al. (1998) J. Biol. Chem. 273, 16351.
    2. Thomas, J.B. et al. (2009) Bioorg. Med. Chem. Lett. 19.5, 1438.
    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 SR 48692 inhibits human NTS1 receptors expressed in CHO-K1 cells.
    Dose-response curve of hNTSR1 normalized inhibition by SR 48692 (#S-265). Cells were loaded with Fluo-8 dye, incubated with increasing concentrations of SR 48692, and stimulated with 3 nM neurotensin. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 0.52 µM.
    References - Scientific Background
    1. Labbe-Jullie, C. et al. (1994) J. Pharmacol. Exp. Ther. 271, 267.
    2. Labbe-Jullie, C. et al. (1998) J. Biol. Chem. 273, 16351.
    3. Thomas, J.B. et al. (2009) Bioorg. Med. Chem. Lett. 19.5, 1438.
    Scientific background

    SR 48692 is a potent and selective antagonist of neurotensin receptor 1 (NTR1/NTS1). The compound demonstrates hydrophobic and aromatic features1,2. SR 48692 has been shown to antagonize neurotensin receptor actions in intestinal preparations, thus considered to be a useful tool in studying the physiological role of neurotensin receptor in the digestive tract. in vitro studies show that SR 48692 antagonizes NT-induced dopamine release in guinea pig striatal slices and NT-stimulated Ca2+ mobilization in HT29 cells1. In guinea pig ileum preparations, the compound displays an IC50 value of 33.5 nM1.

    The two neurotensin receptors, NTR1 and NTR2, belong to the family of G-protein-coupled receptors1,2. The receptors are expressed in the brain and gastrointestinal tract where they play a role in pain transmission and intestinal motility.

    Target Neurotensin Receptor 1

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    Last update: 22/11/2018

    SR 48692 (#S-265) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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