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Sitaxsentan sodium

Chemical Structure : Sitaxsentan sodium

CAS No.: 210421-74-2

Sitaxsentan sodium (TBC-11251 sodium;TBC-11251)

Catalog No.: PC-42811Not For Human Use, Lab Use Only.

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

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Withdrawn

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.

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