A potent ETA receptor antagonist (IC50 = 1.4 nM); selective for ETA over ETB receptors (IC50 = 9

Sitaxentan (sodium salt) – 10 mg

Brand:
Cayman
CAS:
210421-74-2
Storage:
-20
UN-No:
Non-Hazardous - /

Sitaxentan is a potent nonpeptide endothelin A (ETA) receptor antagonist (IC50 = 1.4 nM).{52222} It is selective for ETA over ETB receptors (IC50 = 9,800 nM). Sitaxentan inhibits phosphoinositol hydrolysis induced by endothelin-1 (Item No. 24127) 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.{52223} 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.{52224} Formulations containing sitaxentan have been used in the treatment of hypertension.  

 

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Description

A potent ETA receptor antagonist (IC50 = 1.4 nM); selective for ETA over ETB receptors (IC50 = 9,800 nM); inhibits endothelin-1-induced phosphoinositol hydrolysis in COS-7 cells (pA2 = 8); reduces blood pressure in a rat model of acute hypoxia-induced pulmonary hypertension (ED50 = 0.5 mg/kg); reduces femoral artery neointimal lesion size in a mouse model of intraluminal injury; decreases BALF pleocytosis, as well as pulmonary collagen deposition and fibrosis, and improves lung mechanics in a mouse model of bleomycin-induced lung injury at 15 mg/kg

Formal name: N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonamide, monosodium salt

Synonyms:  TBC 11251|Thelin

Molecular weight: 476.9

CAS: 210421-74-2

Purity: ≥98%

Formulation: A solid

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