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Zibotentan

MCE China：Zibotentan

Brand：MedChemExpress (MCE)

Cat. No.HY-10088

CAS：186497-07-4

Synonyms：ZD4054

Purity：99.17%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.

In Vitro：Zibotentan potently inhibits the binding of 125iodine-ET-1 to cloned human ETA expressed in mouse erythroleukaemic cells, with a pIC50 (concentration to inhibit 50% of binding) value of 22 nM[1]. Zibotentan (48 hours) treatment increases the number of early apoptotic cells in serum-starved A2780 WT cells[2]. Zibotentan (ZD4054; 1 μM; 24 hours) treatment shows significant inhibition of cell proliferation in serum-starved HEY, OVCA 433, SKOV-3, and A-2780 cells[3]. Zibotentan (ZD4054; 1 μM; 48 hours) treatment induces an increase in apoptotic cells. Zibotentan inhibits bcl-2 and activates caspase-3 and poly(ADP-ribose) polymerase proteins.[3]. Zibotentan (ZD4054; 1 μM) decreases the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells[3]. Zibotentan treatment also results in a reduction of ETAR-driven angiogenesis and invasive mediators, such as vascular endothelial growth factor, cyclooxygenase-1/2, and matrix metalloproteinase (MMP)[3].

In Vivo：Zibotentan (10 mg/kg; intraperitoneal injection; daily; for 21 days) treatment significantly inhibits tumor growth in mice. And Zibotentan treatment increases E-cadherin expression[2].

IC50 & Target：ETA 13 nM (Ki)

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References：

[1]. C D Morris, et al. Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br J Cancer. 2005 Jun 20;92(12):2148-52.  [Content Brief]

[2]. Laura Rosanò, et al. Acquisition of chemoresistance and EMT phenotype is linked with activation of the endothelin A receptor pathway in ovarian carcinoma cells. Clin Cancer Res. 2011 Apr 15;17(8):2350-60.  [Content Brief]

[3]. Laura Rosanò, et al. ZD4054, a specific antagonist of the endothelin A receptor, inhibits tumor growth and enhances paclitaxel activity in human ovarian carcinoma in vitro and in vivo. Mol Cancer Ther. 2007 Jul;6(7):2003-11.  [Content Brief]