2. GPCR/G Protein
  3. Endothelin Receptor
  4. Sitaxsentan sodium

Sitaxsentan sodium  (Synonyms: IPI 1040 sodium; TBC11251 sodium)

Cat. No.: HY-11103 Purity: 98.83%
COA Handling Instructions

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Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.

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

Sitaxsentan sodium Chemical Structure

Sitaxsentan sodium Chemical Structure

CAS No. : 210421-74-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in Water USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 110 In-stock
50 mg USD 350 In-stock
100 mg USD 580 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Sitaxsentan sodium:

Sitaxsentan sodium Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Sitaxsentan sodium

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ETA ETB

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.

IC50 & Target

ETB

 

In Vitro

Sitaxsentan and Bosentan attenuate NTCP transport at higher concentrations, and inhibit human hepatic transporters, which provides a potential mechanism for the increased hepatotoxicity observed for these agents in the clinical setting. Only sitaxsentan decreased OATP transport (52%)[1]. Sitaxsentan and sitaxsentan combined with sildenafil completely prevent the increased expressions of endothelin-1 and of the ETB receptor. Sitaxsentan alone partially restores the expressions of BMPR-1A and BMPR-2. The combination of sildenafil and sitaxsentan further restores the expressions of BMPR-1A and BMPR-2, which remaines, however, decreased compared with controls[3].

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

Sitaxsentan sodium Related Antibodies
In Vivo

Sitaxsentan (5 mg/kg infused iv 10 min prior to onset of hypoxia) completely blocks hypoxia-induced vasoconstriction and this group does not differ from air controls. Oral administration of sitaxsentan, significantly attenuates the increase in MPAP, while the administration of sitaxsentan to rats exposed to normal oxygen levels is without effect on MPAP[2]. Sitaxsentan alone limits shunt-induced increase in MT. Sitaxsentan combined with sildenafil more effectively prevents this remodeling, which, however, tends to remain increased compared with controls[3].

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

476.89

Formula

C18H14ClN2NaO6S2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C1=C(SC=C1)C(CC2=C(C=C3OCOC3=C2)C)=O)(N([Na])C4=C(C(C)=NO4)Cl)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (209.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (209.69 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0969 mL 10.4846 mL 20.9692 mL
5 mM 0.4194 mL 2.0969 mL 4.1938 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 33.33 mg/mL (69.89 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 98.83%

COA (263 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2]

After an initial 2-week period of hypoxic exposure (10% O2) sitaxsentan (15 or 30 mg/kg body weight per day in the drinking water) is administered for 4 weeks during continuous exposure to hypoxia. At the conclusion of the 4 week period of hypoxia, femoral and pulmonary arterial cannulation and measurement of MPAP, MSAP, and HR are performed.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.0969 mL 10.4846 mL 20.9692 mL 52.4230 mL
5 mM 0.4194 mL 2.0969 mL 4.1938 mL 10.4846 mL
10 mM 0.2097 mL 1.0485 mL 2.0969 mL 5.2423 mL
15 mM 0.1398 mL 0.6990 mL 1.3979 mL 3.4949 mL
20 mM 0.1048 mL 0.5242 mL 1.0485 mL 2.6211 mL
25 mM 0.0839 mL 0.4194 mL 0.8388 mL 2.0969 mL
30 mM 0.0699 mL 0.3495 mL 0.6990 mL 1.7474 mL
40 mM 0.0524 mL 0.2621 mL 0.5242 mL 1.3106 mL
50 mM 0.0419 mL 0.2097 mL 0.4194 mL 1.0485 mL
60 mM 0.0349 mL 0.1747 mL 0.3495 mL 0.8737 mL
80 mM 0.0262 mL 0.1311 mL 0.2621 mL 0.6553 mL
100 mM 0.0210 mL 0.1048 mL 0.2097 mL 0.5242 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Sitaxsentan sodium 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:

Sitaxsentan210421-74-2IPI 1040TBC11251IPI1040IPI-1040TBC 11251TBC-11251Endothelin ReceptorInhibitorinhibitorinhibit

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