BMS 182874 hydrochloride

A Selective Antagonist of Endothelin A Receptors
    Cat #: B-500
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 381.88
    Purity: >99%
    Effective concentration 100 nM – 10 µM.
      • BMS 182874 hydrochloride
    Chemical name 5-(dimethylamino)-N-(3,4-dimethyl-1,2-oxazol-5-yl)naphthalene-1-sulfonamide;hydrochloride.
    Molecular formula C17H19N3O3S · HCl
    CAS No.: 1215703-04-0.
    PubChem CID 56972163
    Activity BMS 182874 hydrochloride is a potent, selective and competitive antagonist of ET-A endothelin receptors. It exhibits a 1000-fold selectivity for ET-A over ET-B receptors, inhibiting endothelin-1 radioligand binding to ET-A and ET-B with Ki of 61 nM and >50 µM, respectively. In vitro, BMS 182874 inhibits endothelin-1 induced calcium mobilization with KB of 140 nM1. BMS 182874 is orally bioavailable and active in vivo1,2.
      • Webb, M.L. et al. (1995) J. Pharmacol. Exp. Ther. 272, 1124.
      • Holm, P. et al. (1998) Cardiovasc. Res. 37, 765.
    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 +4°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.
      • BMS 182874 hydrochloride
        Alomone Labs BMS 182874 hydrochloride inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
        Dose-response curve of BMS 182874 hydrochloride (#B-500) inhibition of ET-A receptor-mediated, endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 331.2 nM. Cells were loaded with Calcium 6 dye, incubated with BMS 182874 hydrochloride, 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. Webb, M.L. et al. (1995) J. Pharmacol. Exp. Ther. 272, 1124.
    • 2. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
      • BMS 182874 hydrochloride is a synthetic compound that acts as a selective, potent, and competitive antagonist of endothelin A (ET-A) receptors. BMS 182874 exhibits a 1000-fold selectivity for ET-A over ET-B receptors. The compound is a useful tool for understanding the role of endothelin in normal and disease conditions. BMS 182874 inhibits the binding of radioligand binding of ET-1 to ET-A receptors in rat vascular smooth muscle cell membranes with Ki of 61 nM and in Chinese ovary hamster cells with Ki of 48 nM1.

        Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also expressed in several different regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides2.

    Target ET-A receptors
    Last update: 27/08/2019

    BMS 182874 hydrochloride (#B-500) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use