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Sitaxsentan
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Catalog No. T12924Cas No. 184036-34-8
Alias TBC-11251, IPI 1040
Sitaxsentan (TBC-11251) is A selective endothelin A (ETA) receptor antagonist. Endothelin is an effective vasoconstrictor. Sitaxsentan blocks the binding of endothelin to its receptors, thereby eliminating the harmful effects of endothelin.
Sitaxsentan
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Purity: 98.71%
Catalog No. T12924Alias TBC-11251, IPI 1040Cas No. 184036-34-8
Sitaxsentan (TBC-11251) is A selective endothelin A (ETA) receptor antagonist. Endothelin is an effective vasoconstrictor. Sitaxsentan blocks the binding of endothelin to its receptors, thereby eliminating the harmful effects of endothelin.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $300 | In Stock | In Stock | |
| 5 mg | $778 | In Stock | In Stock | |
| 10 mg | $1,000 | In Stock | In Stock | |
| 25 mg | $1,300 | In Stock | In Stock | |
| 50 mg | $1,600 | In Stock | In Stock | |
| 100 mg | $2,000 | In Stock | In Stock | |
| 500 mg | $4,000 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:98.71%
Appearance:Solid
Color:Yellow
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Product Introduction
Sitaxsentan AI Summary
Sitaxsentan exhibits bioactivities related to endothelin receptors, showing potent inhibitory effects on the endothelin A receptor with an IC50 of 1.4 nM and a Ki value of 0.43 nM, and on the endothelin B receptor with an IC50 of 9.8 nM. The compound demonstrates high selectivity for the endothelin A receptor over the endothelin B receptor, with a selectivity value of 7000. Bioavailability studies indicate high oral bioavailability, achieving approximately 80% in humans, 100% in dogs, and 60% in rats. Pharmacokinetic data show a serum half-life ranging from 4.1 to 7.5 hours depending on the species. Additionally, Sitaxsentan shows antiviral activity against SARS-CoV-2, moderate liver toxicity with elevated ALT and AST levels, and moderate inhibitory activity against PDE4A. While demonstrating specific bioactivities, it does not exhibit significant bioactivity for most other targets tested..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Sitaxsentan (TBC-11251) is A selective endothelin A (ETA) receptor antagonist. Endothelin is an effective vasoconstrictor. Sitaxsentan blocks the binding of endothelin to its receptors, thereby eliminating the harmful effects of endothelin. |
| Synonyms | TBC-11251, IPI 1040 |
| Molecular Weight | 454.9 |
| Formula | C18H15ClN2O6S2 |
| Cas No. | 184036-34-8 |
| Smiles | C(CC=1C=C2C(=CC1C)OCO2)(=O)C3=C(S(NC4=C(Cl)C(C)=NO4)(=O)=O)C=CS3 |
| Relative Density. | 1.6g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4.55 mg/mL (10 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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