PD-156707

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.
    Structure
    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™.
    References
    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

    Promotion

    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