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.
    Structure
    • 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.
    References-Activity
    1. Webb, M.L. et al. (1995) J. Pharmacol. Exp. Ther. 272, 1124.
    2. 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.
    Our bioassay
    • 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.
    Scientific background

    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: 24/01/2020

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

    For research purposes only, not for human use

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    Scientific Background

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