Overview
- Morris, C.D. et al. (2005) Br. J. Cancer 92, 2148.
Alomone Labs Zibotentan inhibits ETA receptor-mediated Ca2+ mobilization in CHO cells.Dose response curve of Zibotentan (#Z-130) inhibition of the ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 146.8 nM. Cells were loaded with Calcium 6 dye, incubated with Zibotentan, and stimulated with 15 nM Endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
- Morris, C.D. et al. (2005) Br. J. Cancer 92, 2148.
- Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
Zibotentan (ZD4054) is an orally active nonpeptide with specificity towards Endothelin A (ET-A) receptors with no activity on Endothelin B (ET-B) receptors. The compound inhibits endothelin-1 radioligand binding to human ET-A receptor with an IC50 value of 21 nM1.
Studies show that Zibotentan successfully inhibits growth of tumor xenografts in mice and enhances the cytotoxicity of paclitaxel in ovarian carcinoma in vitro and in vivo1.
Endothelin receptors 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-32.
Zibotentan (#Z-130) is a highly pure, synthetic, and biologically active compound.
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