A Potent and Selective Antagonist of Endothelin A Receptors
  • New
Cat #: P-305
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
  • Promotion
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 528.49 Da.
    Purity >99%.
    Effective concentration 1-100 nM.
    Chemical name Sodium (Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoate.
    Molecular formula C28H25O9·Na.
    CAS number 162412-70-6.
    Activity PD-156707 is a potent and selective antagonist of the ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 0.17 nM and 133.8 nM, respectively. in vitro, PD-156707 inhibits ET-A and ET-B receptor-mediated arterial vasoconstriction with pAof 7.5 and 4.7, respectively. PD-156707 is orally bioavailable and active in vivo1.
    Storage before reconstitution Product before reconstitution should be store desiccated 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-156707 inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
    Dose response plot of PD-156707 (#P-305) inhibition of ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 0.95 nM. hETA-expressing CHO-K1 cells were loaded with Calcium 6 dye, incubated with PD-156707, and stimulated with 15 nM Endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    1. Reynolds, E.E. et al. (1995) J. Pharmacol. Exp. Ther. 273, 1410.
    2. Maguire, J.J. et al. (1997) J. Pharmacol. Exp. Ther. 280, 1102.
    3. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    Target: ET-A receptor


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

    New website special

    Last update: 25/12/2017

    PD-156707 is a synthetic compound that acts as a potent and selective antagonist of Endothelin A receptor (ET-A) subtype. PD-156707 is being used to define the physiological and pathological roles of endothelin A receptors. It demonstrates selectivity for ET-A receptor over ET-B receptor1,2.

    PD-156707 inhibits endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 0.17 nM and 133.8 nM, respectively1 and antagonizes endothelin-1-stimulated phosphoinositide hydrolysis in Ltk cells expressing cloned human endothelin A receptors with an IC50 value of 2.4 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 expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also present in several regions of the brain. 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 equally high affinity for all endothelin isopeptides3.

    Alomone Labs is pleased to offer PD-156707 (#P-305).

    For research purposes only, not for human use