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
SDS
Handling Instructions Technical Support

Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally activeendothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium inhibits ET-1-induced phosphoinositide turnover. Sitaxsentan sodium can significantly alleviate pulmonary arterial hypertension (PAH) symptoms. Sitaxsentan sodium can be used for the study of PAH.

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Sitaxsentan sodium Chemical Structure

Sitaxsentan sodium Chemical Structure

CAS No. : 210421-74-2

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Based on 1 publication(s) in Google Scholar

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Sitaxsentan sodium Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Sitaxsentan sodium

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ETA ETB

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Description

Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally activeendothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium inhibits ET-1-induced phosphoinositide turnover. Sitaxsentan sodium can significantly alleviate pulmonary arterial hypertension (PAH) symptoms. Sitaxsentan sodium can be used for the study of PAH[1][2][3][4][5].

IC50 & Target

ETB

 

In Vitro

Sitaxsentan sodium (100 μM, 10 min) significantly inhibits taurocholate cotransporter (NTCP) and organic anion transporter (OATP) transportation in sandwich-cultured human hepatocytes[3].
Sitaxsentan sodium (10 min) has a high efficiency of liver cell uptake and almost no bile excretion[3].
Sitaxsentan sodium has moderate hepatobiliary transporters bile salt export pump (BSEP) inhibition (IC50 = 25 μM) in sandwich-cultured human hepatocytes[5].

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

Sitaxsentan sodium Related Antibodies
In Vivo

Sitaxsentan sodium (1.5 mg/kg, p.o., three times a day for 3 months) effectively prevents PAH caused by shunt induction, and the combined medication with Sildenafil (HY-15025) has a better effect in piglets[1].
Sitaxsentan sodium (5 mg/kg, i.v., single dose) completely blocks the activation of ETA receptors in the acute hypoxia model of rats[2].
Sitaxsentan sodium (15-30 mg/kg, p.o., once daily for 2-4 weeks) significantly improves PAH and vascular remodeling caused by chronic hypoxia, but has limited effect on the already formed right ventricular hypertrophy in rat chronic hypoxia model[2].
Sitaxsentan sodium (10-50 mg/kg, p.o., once daily for 3 weeks) dose-dependently improves Monocrotaline(HY-N0750)-induced pulmonary hypertension in rats[2].

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

Animal Model: Shunt-induced PAH model established in piglets (18 days old, 5.3 kg)[1]
Dosage: 1.5 mg/kg or 1.5 mg/kg combined with 0.75 mg/kg Sildenafil
Administration: Oral administration (p.o.) with food, three times a day for 3 months
Result: combined treatment completely restored the normal state.
partially inhibited the thickening of blood vessels with single-drug and the combined therapy almost completely prevented it.
Partially restored the expression of BMPR-1A and BMPR-2.
Maintained normal right ventricle-aorta coupling.
Animal Model: Acute hypoxia induced PHA model established in male Sprague-Dawley rats[2]
Dosage: 5 mg/kg
Administration: Intravenous injection (i.v.), 10 minutes before or 50 minutes after the onset of hypoxia
Result: Completely blocked the increase in pressure in prevention group.
Rapidly reversed the elevated MPAP after administration of the drug (reaching normal levels within approximately 30 minutes) in treatment group.
Animal Model: Chronic hypoxia induced PHA model established in male Sprague-Dawley rats[2]
Dosage: 15 mg/kg in prevention group and 15 mg/kg and 30 mg/kg in treatment group
Administration: Oral administration (p.o.) with water, once daily, 48 hours before hypoxia and lasting for 2 weeks or after 2 weeks of hypoxia and lasted for 4 weeks
Result: Decreased The MPAP in the prevention group by 35%, and in the treatment group decreased by 38%.
Reduced the ratio of RV/(LV + S) to some extent.
Improved pulmonary vascular remodeling in both groups.
Animal Model: Monocrotaline induced PHA model established in male Sprague-Dawley rats[2]
Dosage: 10 and 50 mg/kg
Administration: Oral administration (p.o.) with water, once daily for 3 weeks
Result: Improved hemodynamic conditions.
Almost completely prevented pulmonary vascular remodeling at high dose (50mg/kg).
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%

SDS (393 KB)

COA (263 KB) LCMS (96 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, 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

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  • 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 ReceptorAURKANeuroblastomaPROTACMYCNTargeted protein degradationInhibitorinhibitorinhibit

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