Sitaxsentan | ETA receptor inhibitor | Probechem Biochemicals

Chemical Structure : Sitaxsentan

CAS No.: 184036-34-8

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

货号: 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.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥3480	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	454.9045
分子式	C18H15ClN2O6S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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]-

参考文献

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.

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

生物&药学活性

物理化学性质&存储条件

参考文献

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

生物&药学活性

物理化学性质&存储条件

参考文献

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