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sitaxsentan

Names

[ CAS No. ]:
184036-34-8

[ Name ]:
sitaxsentan

[Synonym ]:
Sitaxsentan
Sitax

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor
Research Areas >> Cardiovascular Disease

[References]

[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.


[Related Small Molecules]

BQ-788 (sodium salt) | Endothelin-1 (human, bovine, dog, mouse, porcine, rat) acetate salt | Atrasentan hydrochloride | BQ-123 | Zibotentan (ZD4054) | ACT-132577 | RE 201 | Atrial Natriuretic Factor (1-28) (mouse, rabbit, rat) trifluoroacetate salt | Avosentan | Sitaxentan sodium | IRL-1620 TFA | Sulfisoxazole | Aminaftone | PD-159020 | Ro 46-2005

Chemical & Physical Properties

[ Density]:
1.6g/cm3

[ Boiling Point ]:
600.4ºC at 760 mmHg

[ Molecular Formula ]:
C18H15ClN2O6S2

[ Molecular Weight ]:
454.90500

[ Flash Point ]:
316.9ºC

[ Exact Mass ]:
454.00600

[ PSA ]:
144.35000

[ LogP ]:
5.11500

[ Vapour Pressure ]:
2.25E-14mmHg at 25°C

[ Index of Refraction ]:
1.687

[ Storage condition ]:
2-8℃

Synthetic Route

Precursor & DownStream


Related Compounds