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Ro46-8443

A Selective Antagonist of Endothelin B Receptors

Cat #: R-185
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 609.69
    Purity: >95%
    Effective concentration 0.1-10 µM.
    Structure
    Chemical name 4-tert-butyl-N-[6-[(2R)-2,3-dihydroxypropoxy]-5-(2-methoxyphenoxy)-2-(4-methoxyphenyl)pyrimidin-4-yl]benzenesulfonamide.
    Molecular formula C31H35N3O8S.
    CAS No.: 175556-12-4
    PubChem CID 5312146
    Activity Ro 46-8443 is a non-peptide, selective and competitive antagonist of ET-B receptors. It shows over 100-fold selectivity for human ET-B in competitive binding assays (IC50 of 34-69 nM), and competitively inhibits the binding of selective ET-B agonist [125I]Sarafotoxin-S6c to porcine trachea membranes (IC50 = 4.9 nM)1.
    References-Activity
    1. Breu, V. et al. (1996) FEBS Lett. 383, 37.
    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 -20°C.
    Solubility Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs Ro46-8443 inhibits ETB receptor-mediated Ca2+ mobilization in CHO cells.
      Alomone Labs Ro46-8443 inhibits ETB receptor-mediated Ca2+ mobilization in CHO cells.
      Dose response plot of Ro46-8443 (#R-185) inhibition of the ET-B receptor-mediated, endothelin-1-evoked Ca2+ mobilization (IC50 = 0.88 µM). Cells were loaded with Calcium 6 dye, incubated with Ro46-8443, and stimulated with 30 nM endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    1. Breu, V. et al. (1996) FEBS Lett. 383, 37.
    2. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    3. Xie, C. and Wang, D.H. (2009) Hypertension 54, 1298.
    Scientific background

    Ro46-8443 is a synthetic compound that acts as a selective and competitive antagonist of the ET-B (endothelin B) receptor, a receptor that belongs to the G-protein coupled receptor (GPCR) superfamily. Ro46-8443 shows a 100-fold selectivity for human ET-B over ET-A receptors and is being used as an important tool for studying the role of ET-B receptors in pathology1. Ro 46-8443 demonstrates IC50 values of 34 nM and 69 nM in competitive binding assays for human ET-B receptors in radiolabeled membranes of Chinese hamster ovary cells and microsomal membranes from human placenta, respectively. The compound also inhibits the binding of selective radiolabeled ET-B agonist Sarafotoxin-S6c to porcine trachea membranes with an IC50 value of 4.9 nM1.

    Endothelin receptors are widely distributed in vascular and nonvascular tissues. The ET-B receptor has high and equal affinity for all endothelin isopeptides3. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia3.

    Target ET-B receptor
    Lyophilized Powder
    Last update: 06/11/2022

    Ro46-8443 (#R-185) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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