Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC 50 of 1.4 nM and a K i of 0.43 nM. Sitaxsentan exhibits an IC 50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4 , normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.
Products | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Metabolic or Endocrine Disease | Products > Signaling Pathways > GPCR/G Protein | Products > Signaling Pathways > TGF-beta/Smad | Products > Research Areas > Metabolic Disease | Products > Research Areas > Cardiovascular Disease | Products > Signaling Pathways > Endothelin Receptor | Products > Signaling Pathways > TGF-β Receptor
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