Toggle Nav
Close
  • Menu
  • Setting

Zibotentan (ZD4054)

Catalog No.
A5489
ETA receptor antagonist,potent and specific
Grouped product items
SizePriceStock Qty
1mg
$53.00
In stock
5mg
$181.00
In stock
10mg
$247.00
In stock
25mg
$551.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Zibotentan (ZD4054; CAS 186497-07-4) is a selective antagonist of the endothelin A receptor (ET_AR). The endothelin-1 (ET-1)/ET_AR signaling axis is implicated in ovarian cancer progression. In vitro studies in ET_AR-positive human ovarian cancer cell lines demonstrate that Zibotentan decreases basal and ET-1-stimulated proliferation, suppresses phosphorylation of AKT and p42/44 MAPK, reduces anti-apoptotic protein bcl-2 expression, and elevates active caspase-3 levels, enhancing apoptosis. In vivo, Zibotentan inhibits tumor growth in HEY ovarian carcinoma xenograft models, reducing proliferation index, microvascular density, and MMP-2 expression, and augments paclitaxel's antitumor activity. Clinically, pharmacokinetic assessments in advanced solid tumor patients indicate consistent safety profiles across patient populations.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt424.43
Cas No.186497-07-4
FormulaC19H16N6O4S
Solubilityinsoluble in EtOH; insoluble in H2O; ≥7.2 mg/mL in DMSO
Chemical NameN-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
SDFDownload SDF
Canonical SMILESCC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description Zibotentan (ZD4054) is a specific antagonist of Endothelin (ET)A with an IC50 value of 21 nM.
Targets ETA          
IC50 21 nM          

Quality Control