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Zibotentan Chemical Structure

Zibotentan

Data Sheet For research use only. Not for human use.
Cat. No. :BCP02389CAS No. :186497-07-4Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 186497-07-4 Cat. No. BCP02389
Name Zibotentan
Synonyms ZD4054;ZD 4054;ZD-4054;
SMILES
Chemical Name
Formula C19H16N6O4S M. Wt 424.43
Purity 98% Storage Store at 4-8°C
Description As Zibotentan specifically inhibits ETA-mediated antiapoptotic effects, but not ETB-mediated proapoptotic effects in human and rat smooth muscle cells, Zibotentan binds to endothelin A receptor (ETA) with high affinity with Ki of 13 nM, and has no affinity for endothelin B receptor (ETB) with IC50 of >10 μM. Zibotentan treatment at 1 μM inhibits ET-1 induced mitogenic activity in ovarian carcinoma cell lines HEY and OVCA 433 secreting ET-1 and expressing ETA and ETB mRNA. ZD4054 (1 μM) inhibits ET-1 induced EGFR transactivation in HEY and OVCA 433 cells. Zibotentan (1 μM) reverts ET-1 mediated epithelial-mesenchymal transition (EMT), by enhancing E-cadherin expression and promoter activity, and inhibiting vascular endothelial growth factor (VEGF) secretion and invasiveness in HEY and OVCA 433 cells. Zibotentan also potently inhibits the basal and ET-1 induced cell proliferation in SKOV-3 and A-2780 cells, associated with the inhibition of AKT and p42/44MAPK phosphorylation, and with in
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