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Sitaxsentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki value of 1.4 nM and 0.43 nM, respectively. Sitaxsentan sodium inhibits ET-1-induced stimulation of phosphoinositide turnover with a Ki of 0.69 nM and a pA2 of 8.0. Sitaxsentan blocks the action of endothelin (ET) on the endothelin-A (ETA) receptor selectively (by a factor of 6000 compared to the ETB). Sitaxsentan blocked increased plasma endothelin levels in the prevention protocol but did not affect the established elevated levels in the intervention study.
| Molecular Weight | 476.89 |
| Formula | C18H14ClN2NaO6S2 |
| CAS Number | 210421-74-2 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Endothelin Receptor Products |
|---|
| A-127722
A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ETA selective endothelin receptor (ET receptor) antagonist with IC50 value of 0.36 nM. |
| Endothelin 1 (swine, human) (TFA)
Endothelin 1 (swine, human) (TFA) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. |
| Atrial Natriuretic Peptide (ANP) (1-28), rat
Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner. |
| [Asn18] Endothelin-1, human
[Asn18] Endothelin-1, human is a peptide. |
| [Lys4] Sarafotoxin S6c
[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. |
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