Figure 1: ET-1-induced concentration-dependent stimulation of intracellular calcium mobilization in CHO-K1/EDNRA cells. The cells were loaded with Calcium-4 prior to stimulation with an EDNRA receptor agonist, ET-1. The intracellular calcium change was measured by FLIPRTETRA. The relative fluorescent units (RFU) were recorded and normalized to plot against the log of the cumulative doses of ET-1 (Mean ± SD, n = 2). The EC50 of ET-1 on EDNRA expressing CHO-K1 cells was 2.5 nM.
Note:
1. EC50 value is calculated with four parameter logistic equation:
Y=Bottom + (Top-Bottom)/ (1+10^ ((LogEC50-X)*HillSlope))
X is the logarithm of concentration.
Y is the response and starts at Bottom and goes to Top with a sigmoid shape.
CHO-K1/EDNRA Stable Cell Line
In mammals, the endothelin (ET) family comprises three endogenous isoforms: ET-1, ET-2, and ET-3. These endothelium-derived peptides perform their functions via two endothelin receptors, classified as EDNRA and EDNRB. EDNRA receptors are mainly localized in the vascular smooth muscle cells, where they are the predominant sub-type, and mediate vasoconstriction and proliferation. Selective EDNRA antagonists are effective in the treatment of heart failure, essential hypertension, pulmonary hypertension, and atherosclerosis.
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