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

PD-164333

A Selective Antagonist of Endothelin A Receptors
  • New
    New
  • Bioassay tested
    Bioassay tested
  • Shipped at room temp.
    Shipped at room temp.
  • Cat #: P-310
  • Size: 0.5 mg, 1 mg, 2.5 mg, 5 mg
  • Source: Synthetic
  • MW: 823.63 Da.
  • Target: ET-A receptors
General information


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).
Our Bioassay
Specifications
References
 
Our bioassay
PD-164333 - Alomone Labs PD-164333 inhibits ETA receptor-mediated Ca2+ mobilization in CHO-K1 cells.
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™.
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For research purposes only, not for human use
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