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A-192621

A Selective Antagonist of Endothelin B Receptors

Cat #: A-360
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 558.68
    Purity: >97% (HPLC)
    Effective concentration 0.1-10 nM.
    Structure
    Chemical name (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(2,6-diethylanilino)-2-oxoethyl]-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid.
    Molecular formula C33H38N2O6.
    CAS No.: 195529-54-5
    PubChem CID 5311192
    Activity A-192621 is a selective antagonist of ET-B endothelin receptors, inhibiting ET-1 binding to ETA and ET-3 binding to ETB receptors with IC50 values of 4280 nM and 4.5 nM, respectively1.
    In vivo, A-192621 inhibits ETB-mediated dilatory and pressor responses induced by Sarafotoxin 6c (ED50 = 30 mg/kg), and causes an elevation of arterial blood pressure and plasma ET-1 level2.
    References-Activity
    1. Wu-Wong, J.R. et al. (2002) Clin. Sci. 103, 418S.
    2. Wessale, J.L. et al. (2002) Clin. Sci. 103, 112S.
    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 or NaOH 1Eq. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs A-192621 inhibits ET-B receptor-mediated Ca2+ mobilization in CHO cells.
      Alomone Labs A-192621 inhibits ET-B receptor-mediated Ca2+ mobilization in CHO cells.
      Dose-response plot of A-192621 (#A-360) inhibition of ET-B receptor-mediated, endothelin-1-evoked Ca2+ mobilization. Complete inhibition was attained at 10 nM. Cells were loaded with Calcium 6 dye, incubated with A-192621, 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. Sakai, S. et al. (2016) Life Sci. 159, 116.
    2. Wessale, J.L. et al. (2002) Clin. Sci. 103, 112S.
    3. Wu-Wong, J.R. et al. (2002) Clin. Sci. 103, 418S.
    4. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    5. Xie, C. and Wang, D.H. (2009) Hypertension 54, 1298.
    Scientific background

    A-192621 is a synthetic compound that acts as a selective antagonist of the endothelin B (ET-B) receptor, a member of the G-protein coupled receptor (GPCR) superfamily.

    In vivo efficacy studies showed that A-192621 inhibits ET-1-induced dilatory and pressor responses that are mediated by ET-B. The compound can cause an increase in arterial blood pressure and plasma ET-1 levels1,2. It inhibits ET-B receptors with an IC50 value of 4.5 nM3.

    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 ganglia4,5.

    Target ET-B receptor
    Lyophilized Powder
    Last update: 02/01/2022

    A-192621 (#A-360) 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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