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

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.

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Zibotentan Chemical Structure

Zibotentan Chemical Structure

CAS No. : 186497-07-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Zibotentan Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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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[1][2].

IC50 & Target[1]

ETA

13 nM (Ki)

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].

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

Zibotentan Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (58.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.19%

COA (253 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3561 mL 11.7805 mL 23.5610 mL 58.9025 mL
5 mM 0.4712 mL 2.3561 mL 4.7122 mL 11.7805 mL
10 mM 0.2356 mL 1.1781 mL 2.3561 mL 5.8903 mL
15 mM 0.1571 mL 0.7854 mL 1.5707 mL 3.9268 mL
20 mM 0.1178 mL 0.5890 mL 1.1781 mL 2.9451 mL
25 mM 0.0942 mL 0.4712 mL 0.9424 mL 2.3561 mL
30 mM 0.0785 mL 0.3927 mL 0.7854 mL 1.9634 mL
40 mM 0.0589 mL 0.2945 mL 0.5890 mL 1.4726 mL
50 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1781 mL
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Zibotentan Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zibotentan186497-07-4ZD4054ZD 4054ZD-4054Endothelin ReceptorApoptosisETACRPCanticancerp4244MAPKbcl-2caspase-3Inhibitorinhibitorinhibit

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