Sitaxsentan (sodium)

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].

Product Specifications

CAS Number

[210421-74-2]

Product Name Alternative

IPI 1040 (sodium) ; TBC11251 (sodium)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Endothelin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Sitaxsentan-sodium.html

Purity

98.83

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C18H14ClN2NaO6S2

Molecular Weight

476.89

Precautions

H302, H315, H319, H335

References & Citations

[1]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|[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.|[3]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.|[4]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. |[5]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.