Sitaxsentan

Research use only, not for human use.

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.

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; dispalys >5,000-fold selectivity over ETB receptors; inhibits ET1-induced stimulation of phosphoinositide turnover with Ki of 0.686 nM, and pA2 of 8.0; excellent PK profile and oral bioavailability.Hypertension Withdrawn.

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IPI-1040 | Sitaxentan | TBC-11251

GPCR/G Protein

Endothelin Receptor

Endothelin Receptor

Cardiovascular Disease

Hypertension

184036-34-8

454.9045

C18H15ClN2O6S2

>98% (HPLC)

10 mM in DMSO

CC1=CC2=C(C=C1CC(=O)C3=C(C=CS3)S(=O)(=O)NC4=C(C(=NO4)C)Cl)OCO2

3-Thiophenesulfonamide, N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-

(-20℃)

With Ice Pack

≥ 2 years