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

BMS 182874 hydrochloride

A Selective Antagonist of Endothelin A Receptors
  • New
    New
  • Bioassay tested
    Bioassay tested
  • Shipped at room temp.
    Shipped at room temp.
  • Cat #: B-500
  • Size: 5 mg, 10 mg, 25 mg, 50 mg
  • Source: Synthetic
  • MW: 381.88 Da.
  • Target: ET-A receptors
General information


BMS 182874 hydrochloride, is a synthetic compound that acts as a selective, potent, and competitive antagonist of endothelin A (ET-A) receptors. BMS 182874 exhibits a 1000-fold selectivity for ET-A over ET-B receptors. The compound is useful tool for understanding the role of endothelin in normal and disease conditions. BMS 182874 inhibits the binding of radioligand binding of ET-1 to ET-A receptors in rat vascular smooth muscle cell membranes with Ki of 61 nM and in Chinese ovary hamster cells with Ki of 48 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 detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also expressed in several different regions of the brain. ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while ET-B receptor has high affinity equally for all endothelin isopeptides2.
 
Alomone Labs is pleased to offer BMS 182874 hydrochloride (#B-500).
Our Bioassay
Specifications
References
 
Our bioassay
BMS_182874_hydrochloride - Alomone Labs BMS 182874 hydrochloride inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
Alomone Labs BMS 182874 hydrochloride inhibits ET-A receptor-mediated Ca2+ mobilization in CHO cells.
Dose response curve of BMS 182874 hydrochloride (#B-500) inhibition of ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 331.2 nM. Cells were loaded with Calcium 6 dye, incubated with BMS 182874 hydrochloride, 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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