Date published: 2026-4-30

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Hydroxy Bosentan (CAS 253688-60-7)

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Alternate Names:
4-(2-Hydroxy-1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2?-bipyrimidin]-4-yl]-benzenesulfonamide
Application:
Hydroxy Bosentan is a metabolite of Bosentan and a mixed endothelin receptor antagonist
CAS Number:
253688-60-7
Purity:
98%
Molecular Weight:
567.61
Molecular Formula:
C27H29N5O7S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Hydroxy Bosentan is a chemical compound that functions as an endothelin receptor antagonist. It interacts with cellular components by specifically targeting and blocking the endothelin receptors, particularly the endothelin type A (ETA) and type B (ETB) receptors. By doing so, it disrupts the binding of endothelin, a potent vasoconstrictor, to its receptors on smooth muscle cells, leading to vasodilation. This mechanism of action ultimately results in the relaxation of blood vessels, particularly in the pulmonary vasculature, and reduces the resistance to blood flow. Additionally, Hydroxy Bosentan may act to inhibit the proliferation of smooth muscle cells, which is beneficial in conditions characterized by abnormal cell growth, such as pulmonary arterial hypertension. Furthermore, it has been observed to reduce inflammation and oxidative stress in the vasculature, contributing to its overall vasodilatory effects. In summary, Hydroxy Bosentan exerts its functional role by antagonizing endothelin receptors, leading to vasodilation, inhibition of smooth muscle cell proliferation, and reduction of inflammation and oxidative stress in the vasculature.


Hydroxy Bosentan (CAS 253688-60-7) References

  1. Absorption, excretion, and metabolism of the endothelin receptor antagonist bosentan in healthy male subjects.  |  Weber, C., et al. 1999. Drug Metab Dispos. 27: 810-5. PMID: 10383925
  2. Influence of severe renal dysfunction on the pharmacokinetics and metabolism of bosentan, a dual endothelin receptor antagonist.  |  Dingemanse, J. and van Giersbergen, PL. 2002. Int J Clin Pharmacol Ther. 40: 310-6. PMID: 12139208
  3. No influence of the endothelin receptor antagonist bosentan on basal and indomethacin-induced reduction of cerebral blood flow in pigs.  |  Rasmussen, M., et al. 2003. Acta Anaesthesiol Scand. 47: 200-7. PMID: 12631050
  4. Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil.  |  Treiber, A., et al. 2007. Drug Metab Dispos. 35: 1400-7. PMID: 17496208
  5. Development of a cell-based high-throughput assay to screen for inhibitors of organic anion transporting polypeptides 1B1 and 1B3.  |  Gui, C., et al. 2010. Curr Chem Genomics. 4: 1-8. PMID: 20448812
  6. Development and validation of a fully automated online human dried blood spot analysis of bosentan and its metabolites using the Sample Card And Prep DBS System.  |  Ganz, N., et al. 2012. J Chromatogr B Analyt Technol Biomed Life Sci. 885-886: 50-60. PMID: 22227055
  7. Phase I and II metabolism and MRP2-mediated export of bosentan in a MDCKII-OATP1B1-CYP3A4-UGT1A1-MRP2 quadruple-transfected cell line.  |  Fahrmayr, C., et al. 2013. Br J Pharmacol. 169: 21-33. PMID: 23387445
  8. Association of CYP2C9*2 with bosentan-induced liver injury.  |  Markova, SM., et al. 2013. Clin Pharmacol Ther. 94: 678-86. PMID: 23863877
  9. Desmethyl bosentan displays a similar in vitro interaction profile as bosentan.  |  Weiss, J., et al. 2015. Pulm Pharmacol Ther. 30: 80-6. PMID: 25535031
  10. Pharmacokinetic interactions among imatinib, bosentan and sildenafil, and their clinical implications in severe pulmonary arterial hypertension.  |  Renard, D., et al. 2015. Br J Clin Pharmacol. 80: 75-85. PMID: 25581063
  11. Analysis of the Metabolic Pathway of Bosentan and of the Cytotoxicity of Bosentan Metabolites Based on a Quantitative Modeling of Metabolism and Transport in Sandwich-Cultured Human Hepatocytes.  |  Matsunaga, N., et al. 2016. Drug Metab Dispos. 44: 16-27. PMID: 26502773
  12. A bosentan pharmacokinetic study to investigate dosing regimens in paediatric patients with pulmonary arterial hypertension: FUTURE-3.  |  Berger, RMF., et al. 2017. Br J Clin Pharmacol. 83: 1734-1744. PMID: 28213957
  13. Comparison of the inhibitory effect of ketoconazole, voriconazole, fluconazole, and itraconazole on the pharmacokinetics of bosentan and its corresponding active metabolite hydroxy bosentan in rats.  |  Chen, M., et al. 2020. Xenobiotica. 50: 280-287. PMID: 31199171
  14. Population pharmacokinetic model to generate mechanistic insights in bile acid homeostasis and drug-induced cholestasis.  |  de Bruijn, VMP., et al. 2022. Arch Toxicol. 96: 2717-2730. PMID: 35876888

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Hydroxy Bosentan, 1 mg

sc-211603
1 mg
$430.00