FR 139317

A Selective Antagonist of Endothelin A Receptors
    Cat #: F-180
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 604.75
    Purity: >99%
    Effective concentration 1 nM – 1 µM.
      • FR 139317
    Chemical name (2R)-2-[[(2R)-2-[[(2S)-2-(azepane-1-carbonylamino)-4-methylpentanoyl]amino]-3-(1-methylindol-3-yl)propanoyl]amino]-3-pyridin-2-ylpropanoic acid.
    Molecular formula C33H44N6O5.
    CAS No.: 142375-60-8.
    PubChem CID 107810
    Activity FR 139317 is a potent and selective antagonist of ET-A receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B with Ki of 1 nM and 7.3 µM, respectively1in vitro, FR 139317 shifted Endothelin-1-induced contractile response curve to the right with pAof 7.2 in isolated rabbit aorta2.
      • Aramori, I. et al. (1993) Mol. Pharmacol. 43, 127.
      • Sogabe, K. et al. (1993) J. Pharmacol. Exp. Ther264, 1040.
    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 desiccated at -20°C.
    Solubility Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
      • FR 139317
        Alomone Labs FR 139317 inhibits ET-A receptor-mediated Ca2+ mobilization in CHO-K1 cells.
        Dose-response curve of FR 139317 (#F-180) inhibition of ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 25.97 nM. Cells were loaded with Calcium 6 dye, incubated with FR 139317, and stimulated with 15 nM Endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
      • FR 139317 is a synthetic linear tripeptide that acts as a potent, competitive and highly selective antagonist of endothelin A (ET-A) receptors. FR 139317 can be used as a useful tool to investigate the physiological properties of ET-A receptor and to explore its role in diseases1,2. FR139317 inhibits the specific binding of radio labeled endothelin 1 to porcine aortic microsomes in a concentration-dependent, monophasic manner with an IC50 value of 0.53 nM2.

        Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. The ET-A receptor has a high specificity towards endothelin-1 and endothelin-2. It is expressed in vascular smooth muscle cells and mediates vasoconstriction3.

    Target ET-A receptors
    Last update: 18/07/2019

    FR 139317 (#F-180) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use