1. GPCR/G Protein
    Apoptosis
  2. Endothelin Receptor
    Apoptosis
  3. Zibotentan

Zibotentan (Synonyms: ZD4054)

Cat. No.: HY-10088 Purity: 99.66%
Handling Instructions

Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a pIC50 of 21 nM and 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.

For research use only. We do not sell to patients.

Zibotentan Chemical Structure

Zibotentan Chemical Structure

CAS No. : 186497-07-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 960 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1620 In-stock
Estimated Time of Arrival: December 31
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Description

Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a pIC50 of 21 nM and 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[1][2].

IC50 & Target[1]

ETA

21 nM (pIC50)

ETA

13 nM (Ki)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

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[3]

Cell Line: HEY and OVCA 433 cells
Concentration: 1 μM
Incubation Time: 48 hours
Result: Induced an increase in apoptotic cells.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic (nu+/nu+) mice (4-6 week of age) injected with wild-type A2780 cells[2]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; daily ; for 21 days
Result: Showed significant inhibition in tumor growth in mice.
Clinical Trial
Molecular Weight

424.43

Formula

C₁₉H₁₆N₆O₄S

CAS No.

186497-07-4

SMILES

O=S(NC1=NC=C(C)N=C1OC)(C2=CC=CN=C2C3=CC=C(C4=NN=CO4)C=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (58.90 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3561 mL 11.7805 mL 23.5610 mL
5 mM 0.4712 mL 2.3561 mL 4.7122 mL
10 mM 0.2356 mL 1.1781 mL 2.3561 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ZibotentanZD4054ZD 4054ZD-4054Endothelin ReceptorApoptosisETACRPCanticancerp4244MAPKbcl-2caspase-3Inhibitorinhibitorinhibit

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Zibotentan
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