SR 48527

SR48527
A Potent and Selective Antagonist of Neurotensin Receptor 1
  • New
Cat #: S-225
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 549
    Purity: >95%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name (2S)-2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]-2-cyclohexylacetic acid.
    Molecular formula C29H29ClN4O5.
    CAS No.: 156579-04-3.
    Activity SR 48527, an analog of SR 48692, is a potent and selective antagonist of NTS1 receptors, shown to inhibit neurotensin-stimulated IP production with Ki of 24 nM1,2.
    References - Activity
    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.
    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 48527 inhibits human NTS1 receptors expressed in CHO-K1 cells.
    Dose-response curve of hNTSR1 normalized inhibition by SR 48527 (#S-225). Cells were loaded with Fluo-8 dye, incubated with increasing concentrations of SR 48527, 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 0.72 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.
    Scientific background

    SR 48527 is a potent and selective antagonist of neurotensin receptor 1 (NTR1/NTS1). It is an analog of SR 48692 and inhibits neurotensin-stimulated IP production with a Ki value of 24 nM1,2.

    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 48527 (#S-225) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Citations
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