Zibotentan
Based on 1 publication(s) in Google Scholar
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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- Purity: 99.37%
- CAS No.: 186497-07-4
- 화학식: C19H16N6O4S
- 분자량:424.43
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Zibotentan
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Biological Activity
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ETA 13 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>100 nM
Compound: 86
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Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
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[PMID: 27321813] |
| CHO | IC50 |
21 nM
Compound: 86
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Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
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[PMID: 27321813] |
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.
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Cell Line:HEY, OVCA 433, SKOV-3, and A-2780 cells
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Concentration:1 μM
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Incubation Time:24 hours
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Result:Showed significant inhibition of cell proliferation.
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Cell Line:HEY and OVCA 433 cells
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Concentration:1 μM
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Incubation Time:48 hours
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Result:Induced an increase in apoptotic cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic (nu+/nu+) mice (4-6 week of age) injected with wild-type A2780 cells[2]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; daily ; for 21 days
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Result:Showed significant inhibition in tumor growth in mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 186497-07-4
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Appearance Solid
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분자량 424.43
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화학식 C19H16N6O4S
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Color White to off-white
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SMILES
O=S(NC1=NC=C(C)N=C1OC)(C2=CC=CN=C2C3=CC=C(C4=NN=CO4)C=C3)=O
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Synonyms
ZD4054
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Expert Opin Drug Discov
In-silico guided identification and in-vitro studies of potential FFAR4 agonists for type 2 diabetes mellitus therapy. [Abstract]2025 Aug;20(8):1075-1092. PMID: 40580106
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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]
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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