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Chemical Structure : Sitaxsentan
CAS No.: 184036-34-8
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $78 | In stock | |
| 10 mg | $118 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $348 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 454.9045 | |
| Formula | C18H15ClN2O6S2 | |
| 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]- |
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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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