Sitaxentan sodium

Base Information

• Chemical Name: Sitaxentan sodium
• CAS No.: 210421-74-2
• Molecular Formula: C18H14ClN2NaO6S2
• Molecular Weight: 476.89
• Mol file: 210421-74-2.mol

Synonyms:4-Chloro-3-methyl-5-(2-(2-(6-methyl-1,3-benzodioxol-5-yl)acetyl)-3-thienylsulfonamido)isoxazole sodium salt;TBC-11251;Thelin;3-Thiophenesulfonamide, N-(4-chloro-3-methyl-5-isoxazolyl)-2-((6-methyl-1,3-benzodioxol-5-yl)acetyl)-, sodium salt;

Chemical Property of Sitaxentan sodium

Chemical Property:

• PSA: 135.56000
• LogP: 4.90080
• Storage Temp.: room temp
• Solubility.: H2O: soluble10mg/mL (clear solution)

Purity/Quality:

99% ^*data from raw suppliers

SitaxsentanSodium ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

• Description: In November Encysive Pharmaceuticals launched Thelin? (sitaxsentan sodium) in the U.K. for the treatment of pulmonary arterial hypertension (PAH), following European Commission approval in August 2006. Sitaxsentan is the first selective endothelin A (ETA) receptor antagonist, and the first once-daily oral treatment available for patients with PAH. It is 6,500-fold selective in the targeting of ETA versus ETB receptors. Sitaxsentan is indicated for improving exercise capacity in PAH patients classified as World Health Organization (WHO) functional class III. Efficacy has been shown in primary pulmonary hypertension and pulmonary hypertension associated with connective tissue disease. In the U.S., Encysive has submitted a complete response to an approvable letter received from the FDA in July. Sitaxentan is a potent nonpeptide endothelin A (ETA) receptor antagonist (IC50 = 1.4 nM). It is selective for ETA over ETB receptors (IC50 = 9,800 nM). Sitaxentan inhibits phosphoinositol hydrolysis induced by endothelin-1 in COS-7 cells (pA2 = 8). In vivo, sitaxentan reduces blood pressure in a rat model of acute hypoxia-induced pulmonary hypertension (ED50 = 0.5 mg/kg). It reduces femoral artery neointimal lesion size in a mouse model of intraluminal injury. Sitaxentan (15 mg/kg) decreases bronchoalveolar lavage fluid (BALF) pleocytosis, as well as pulmonary collagen deposition and fibrosis, and improves lung mechanics in a mouse model of bleomycin-induced lung injury. Formulations containing sitaxentan have been used in the treatment of hypertension.
• Uses: Selective endothelin A (ETA) receptor antagonist. Antihypertensive. Used in treatment of chronic heart failure.