BMS 182874 hydrochloride

A Selective Antagonist of Endothelin A Receptors
  • New
Cat #: B-500
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 381.88 Da.
    Purity >99%.
    Effective concentration 100 nM – 10 µM.
    Structure
    Chemical name 5-(dimethylamino)-N-(3,4-dimethyl-1,2-oxazol-5-yl)naphthalene-1-sulfonamide;hydrochloride.
    Molecular formula C17H19N3O3S · HCl
    CAS number 1215703-04-0.
    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.
    Storage before reconstitution Product before reconstitution should be stored at +4oC.
    Reconstitution Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage after reconstitution Up to three months at -20°C.
    Our bioassay
    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
    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.
    Target: ET-A receptors
    Last update: 08/02/2018

    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 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. ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while ET-B receptor has high affinity equally for all endothelin isopeptides2.

    Alomone Labs is pleased to offer BMS 182874 hydrochloride (#B-500).

    For research purposes only, not for human use