PD-164333

A Selective Antagonist of Endothelin A Receptors
  • New
Cat #: P-310
Sizes: 0.5 mg, 1 mg, 2.5 mg, 5 mg
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  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 823.63 Da.
    Purity >98%.
    Effective concentration 1-100 nM.
    Structure
    Chemical name (Z)-2-(1,3-benzodioxol-5-yl)-3-[[3-[4-[2-(4-hydroxy-3-iodophenyl)ethylamino]-4-oxobutoxy]-4,5-dimethoxyphenyl]methyl]-4-(4-methoxyphenyl)-4-oxobut-2-enoic acid.
    Molecular formula C39H38INO11.
    CAS number Not available.
    Activity PD-164333 is a selective antagonist of the ET-A receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Kd of 0.99 nM and 2.41 µM, respectively. in vitro, PD164333 shifts Endothelin-1 concentration-response curve to the right with pA2 of 8.84 in isolated human saphenous vein1.
    Storage before reconstitution Product before reconstitution should be stored at -20oC.
    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 PD-164333 inhibits ETA receptor-mediated Ca2+ mobilization in CHO-K1 cells.
    Dose response curve of PD-164333 (#P-310) inhibition of the ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 7.59 nM.
    Cells were loaded with Calcium 6 dye, incubated with PD164333, 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. Davenport, A.P. et al. (1998) Br. J. Pharmacol. 123, 223.
    2. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    Target: ET-A receptors

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    Use code: new-yl30-18
    Valid until January 31st, 2018.

    New website special

    Last update: 25/12/2017

    PD-164333 is a synthetic compound that acts as a selective antagonist of ET-A endothelin receptor based on the butenolide series1. It inhibits the binding of radioligand endothelin-1 to left ventricle in a biphasic manner with a KD value of 0.99 nM and 2.41 µM towards ET-A and ET-B, respectively1.

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

    Alomone Labs is pleased to offer PD-164333 (#P-310).

    For research purposes only, not for human use