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Sitaxsentan

Chemical Structure : Sitaxsentan

CAS No.: 184036-34-8

Sitaxsentan (IPI-1040, Sitaxentan, TBC-11251)

Catalog No.: PC-45971Not For Human Use, Lab Use Only.

Sitaxsentan (IPI-1040, Sitaxentan) 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Sitaxsentan (IPI-1040, Sitaxentan) 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 dispalys >5,000-fold selectivity over ETB receptors.
Sitaxsentan inhibits ET1-induced stimulation of phosphoinositide turnover with Ki of 0.686 nM, and pA2 of 8.0.
Sitaxsentan shows excellent PK profile and oral bioavailability.

Physicochemical Properties

M.Wt 454.9045
Formula C18H15ClN2O6S2
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]-

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.

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