Chemical Structure : Sitaxsentan sodium
CAS No.: 210421-74-2
Catalog No.: PC-42811Not For Human Use, Lab Use Only.
Sitaxsentan sodium (TBC11251, IPI 1040) is a potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.
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Sitaxsentan sodium (TBC11251, IPI 1040) is a potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.
Sitaxsentan sodium dispalys >5,000-fold selectivity over ETB receptors.
Sitaxsentan sodium inhibits ET1-induced stimulation of phosphoinositide turnover with Ki of 0.686 nM, and pA2 of 8.0.
Sitaxsentan sodium has excellent PK profile and oral bioavailability.
M.Wt | 476.8863 | |
Formula | C18H14ClN2NaO6S2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
3-Thiophenesulfonamide, N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-, sodium salt (1:1) |
1. Wu C, et al. J Med Chem. 1997 May 23;40(11):1690-7.
2. Wanebo JE, et al. Neurosurgery. 1998 Dec;43(6):1409-17; discussion 1417-8.
3. Tilton RG, et al. Pulm Pharmacol Ther. 2000;13(2):87-97.
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