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.
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.
Physicochemical Properties
M.Wt
476.8863
Formula
C18H14ClN2NaO6S2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
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)
References
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.
