Catalog No.S3034 Synonyms: TBC-11251
Molecular Weight(MW): 476.89
Sitaxentan sodium is a selective endothelin A receptor (ETA) antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively, exhibits 7000-fold selectivity over ETB. Phase 3.
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|Description||Sitaxentan sodium is a selective endothelin A receptor (ETA) antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively, exhibits 7000-fold selectivity over ETB. Phase 3.|
Sitaxentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0. 
|In vivo||Sitaxentan sodium has a serum half-life in the rat and the dog of 6 hours - 7 hours and 60−100% oral bioavailability. Orally administered Sitaxentan sodium is rapidly absorbed in both the rat and the dog with a t1/2(abs) of 0.7 hours and 0.3 hours, respectively. Peak plasma concentrations occurred between 2 hours and 3 hours postdosing in the rat and between 45 minutes and 90 minutes in the dog.  The pulmonary vasoconstrictor response to acute hypoxia (10% O2 for 90 minutes) is prevented with Sitaxentan sodium (5 mg/kg infused i.v. 10 minutes prior to the onset of hypoxia). Sitaxentan sodium delivered i.v. 50 minutes after the onset of hypoxia reverses the established pulmonary vasoconstriction. Sitaxsentan blocks increased plasma endothelin levels. Sitaxsentan dose dependently (10 mg/kg and 50 mg/kg per day in the drinking water) attenuates right ventricular systolic pressure, right heart hypertrophy, and pulmonary vascular remodeling observed 3 weeks after a single subcutaneous injection of monocrotaline.  Systemic administration of the ETA receptor antagonist Sitaxentan sodium significantly attenuates cerebral vasospasm after subarachnoid hemorrhage (SAH).  Sitaxentan sodium reduces the development of hypoxic pulmonary vasoconstriction (HPV) in the pig. In addition, bolus injection of Sitaxentan sodium reverses already established HPV. |
Ligand binding studies:Binding studies are performed in a 30 mM HEPES buffer, pH 7.4, containing 150 mM NaCl, 5 mM MgCl2, and 0.05% bacitracin using 2 mg/tube (ETA) or 0.75 mg/tube (ETB) membrane. Sitaxentan sodium is dissolved in DMSO and diluted with the assay buffer to give a final concentration of 0.25% DMSO. Competitive inhibition experiments are performed in triplicate in a final volume of 200 μL containing 4 pM [125I]ET-1 (1.6 nCi). Nonspecific binding is determined in the presence of 100 nM ET-1. Samples are incubated for 16 hours−18 hours at 24 °C. One milliliter of PBS is then added and the assay centrifuged at 2000 g for 25 minutes at 4 °C. The supernatant is decanted and the membrane bound radioactivity counted on a Genesys gamma counter.
|In vitro||DMSO||40 mg/mL (83.87 mM)|
|Ethanol||20 mg/mL (41.93 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01251848||Withdrawn||Pulmonary Arterial Hypertension||Pfizer||January 2011||Phase 1|
|NCT01210443||Terminated||Hypertension, Pulmonary||Pfizer||November 2010||Phase 3|
|NCT01244620||Terminated||Pulmonary Arterial Hypertension||Pfizer||November 2010||Phase 1|
|NCT01204853||Terminated||Hypertension, Pulmonary||Pfizer||August 2010||Phase 3|
|NCT00995566||Terminated||Pulmonary Arterial Hypertension||Pfizer||April 2010||--|
|NCT01445873||Completed||Pulmonary Arterial Hypertension||Pfizer||December 2009||--|
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