Zibotentan

Research use only, not for human use.

Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.

Zibotentan (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.

Zibotentan potently inhibits the binding of 125iodine-ET-1 to cloned human ETA expressed in mouse erythroleukaemic cells, with apIC50 (concentration to inhibit 50% of binding) value of 22 nM.Zibotentan (48 hours) treatment increases the number of early apoptotic cells in serum-starved A2780 WT cells.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.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..Zibotentan (ZD4054; 1 μM) decreases the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells.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).Cell Proliferation Assay Cell Line:HEY, OVCA 433, SKOV-3, and A-2780 cells.Concentration:1 μM Incubation Time:24 hours Result:Showed significant inhibition of cell proliferation.Apoptosis Analysis Cell Line:HEY and OVCA 433 cells Concentration:1 μM Incubation Time:48 hours Result:Induced an increase in apoptotic cells.

Zibotentan (10 mg/kg; intraperitoneal injection; daily; for 21 days) treatment significantly inhibits tumor growth in mice. And Zibotentan treatment increases E-cadherin expression. Animal Model:Female athymic (nu+/nu+) mice (4-6 week of age) injected with wild-type A2780 cells Dosage:10 mg/kg Administration:Intraperitoneal injection; daily ; for 21 days Result:Showed significant inhibition in tumor growth in mice.

ZD4054

GPCR/G Protein

Endothelin Receptor

ET-A

Cancer

Prostate Cancer

186497-07-4

424.43

C??H??N?O?S

>98% (HPLC)

DMSO:23 mg/mL (54.2 mM); Ethanol:<1 mg/mL; Water:<1 mg/mL

O=S(C1=CC=CN=C1C2=CC=C(C3=NN=CO3)C=C2)(NC4=NC=C(C)N=C4OC)=O

2-(4-(1,3,4-oxadiazol-2-yl)phenyl)-N-(3-methoxy-5-methylpyrazin-2-yl)pyridine-3-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years