Sitaxsentan sodium
Based on 2 publication(s) in Google Scholar
Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin 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 is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.
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- Reinheit: 98.83%
- CAS. Nr.: 210421-74-2
- Formel: C18H14ClN2NaO6S2
- Molecular Weight:476.89
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Sitaxsentan sodium
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Biologische Aktivität
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ETA 1.4 nM (IC50) |
ETA 0.43 nM (Ki) |
ETB 9800 nM (IC50) |
Sitaxsentan (100 μM, 10 min) sodium significantly inhibits taurocholate cotransporter (NTCP) and organic anion transporter (OATP) transportation in sandwich-cultured human hepatocytes[3].
Sitaxsentan (10 min) sodium 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 (5 mg/kg, i.v., single dose) sodium completely blocks the activation of ETA receptors in the acute hypoxia model of rats[2].
Sitaxsentan (15-30 mg/kg, p.o., once daily for 2-4 weeks) sodium 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 (10-50 mg/kg, p.o., once daily for 3 weeks) sodium 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.
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Animal Model:Shunt-induced PAH model established in piglets (18 days old, 5.3 kg)[1]
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Dosage:1.5 mg/kg or 1.5 mg/kg combined with 0.75 mg/kg Sildenafil
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Administration:Oral administration (p.o.) with food, three times a day for 3 months
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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.
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Animal Model:Acute hypoxia induced PHA model established in male Sprague-Dawley rats[2]
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Dosage:5 mg/kg
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Administration:Intravenous injection (i.v.), 10 minutes before or 50 minutes after the onset of hypoxia
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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.
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Animal Model:Chronic hypoxia induced PHA model established in male Sprague-Dawley rats[2]
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Dosage:15 mg/kg in prevention group and 15 mg/kg and 30 mg/kg in treatment group
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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
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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.
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Animal Model:Monocrotaline induced PHA model established in male Sprague-Dawley rats[2]
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Dosage:10 and 50 mg/kg
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Administration:Oral administration (p.o.) with water, once daily for 3 weeks
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Result:Improved hemodynamic conditions.
Almost completely prevented pulmonary vascular remodeling at high dose (50mg/kg).
Chemical Information
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CAS. Nr. 210421-74-2
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Appearance Solid
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Molecular Weight 476.89
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Formel C18H14ClN2NaO6S2
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Color Light yellow to yellow
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SMILES
O=S(C1=C(SC=C1)C(CC2=C(C=C3OCOC3=C2)C)=O)(N([Na])C4=C(C(C)=NO4)Cl)=O
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Synonyms
IPI 1040 sodium; TBC11251 sodium
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Adv Res
Conjugated bile acids facilitate cholangiocyte senescence to promote cholestatic liver diseases via STING signaling. [Abstract]2026 Mar 12:S2090-1232(26)00239-0. PMID: 41831676 -
Biotechnol Bioeng
An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]2021 Dec;118(12):4687-4698. PMID: 34478150
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (69.89 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (291 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Rondelet B, et al. Sildenafil added to sitaxsentan in overcirculation-induced pulmonary arterial hypertension. Am J Physiol Heart Circ Physiol. 2010 Oct;299(4):H1118-23. Epub 2010 Aug 6. [Content Brief]
[2]. Tilton RG, et al. Attenuation of pulmonary vascular hypertension and cardiac hypertrophy with sitaxsentan sodium, an orally active ET(A) receptor antagonist. Pulm Pharmacol Ther. 2000;13(2):87-97. [Content Brief]
[3]. Hartman JC, et al. Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes. Can J Physiol Pharmacol. 2010 Jun;88 [Content Brief]
[4]. Wu C, et al. Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J Med Chem. 1997 May 23;40(11):1690-7. [Content Brief]
[5]. Lepist EI, et al. Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes. PLoS One. 2014 Jan 30;9(1):e87548. [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, 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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