Sitaxsentan

Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure. IC50 value: Target: ETA receptor

Product Specifications

CAS Number

[184036-34-8]

Product Name Alternative

IPI 1040; TBC-11251

UNSPSC

12352005

Hazard Statement

H315-H319-H320

Target

Endothelin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cardiovascular Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/sitaxsentan.html

Solubility

10 mM in DMSO

Smiles

O=S(C1=C(C(CC2=CC3=C(C=C2C)OCO3)=O)SC=C1)(NC4=C(C(C)=NO4)Cl)=O

Molecular Formula

C18H15ClN2O6S2

Molecular Weight

454.90

Precautions

P264-P280-P302+P352-P305+P351+P338-P362

References & Citations

[1]Chin M, Levy RD, Yoshida EM, Byrne MF.Sitaxsentan-induced acute severe hepatitis treated with glucocorticoid therapy.Can Respir J. 2012 Jan-Feb;19 (1) :e1-2.|[2]Sandoval J, et al. STRIDE-4 investigators.Safety and efficacy of sitaxsentan 50 and 100 mg in patients with pulmonary arterial hypertension.Pulm Pharmacol Ther. 2012 Feb;25 (1) :33-9. Epub 2011 Nov 2.|[3]Safdar Z. Effect of transition from sitaxsentan to ambrisentan in pulmonary arterial hypertension.Vasc Health Risk Manag. 2011;7:119-24. Epub 2011 Mar 2.|[4]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.|[5]Kaehler, et al. Successful treatment of portopulmonary hypertension with the selective endothelin receptor antagonist Sitaxentan. Wien Klin Wochenschr. 2011 Apr;123 (7-8) :248-52. Epub 2011 Mar 31.