SR 48527

SR48527
A Potent and Selective Antagonist of Neurotensin Receptor 1
Cat #: S-225
Alternative Name SR48527
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 549
    Purity: >95%
    Effective concentration 1 nM – 1 µM.
    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.
    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 Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
      • 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.
      • 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
    Last update: 11/03/2019

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

    For research purposes only, not for human use
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