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G-Protein Coupled Receptors >> Endothelin Receptors >> Antagonists

PD-156707

A Potent and Selective Antagonist of Endothelin A Receptors
  • New
    New
  • Bioassay tested
    Bioassay tested
  • Shipped at room temp.
    Shipped at room temp.
  • Cat #: P-305
  • Size: 5 mg, 10 mg, 25 mg, 50 mg
  • Source: Synthetic
  • MW: 528.49 Da.
  • Target: ET-A receptor
General information

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).
Our Bioassay
Specifications
References
 
Our bioassay
PD-156707 - Alomone Labs PD-156707 inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
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™.
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For research purposes only, not for human use
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