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.
    Structure
    • 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.
    References-Activity
    1. Aramori, I. et al. (1993) Mol. Pharmacol. 43, 127.
    2. 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.
    Our bioassay
    • 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
    1. Aramori, I. et al. (1993) Mol. Pharmacol. 43, 127.
    2. Peter, M.G. and Davenport, A.P. (1996) Br. J. Pharmacol. 117, 455.
    3. Takase, H. et al. (1995) Hypertension 25, 739.
    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: 24/01/2020

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

    For research purposes only, not for human use
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