Soraprazan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Soraprazan (BYK61359) 是选择性的钾通道竞争性的 H,K-ATPase (Ki=6.4 nM)的抑制剂，在胃腺的 IC50 为 0.19 μM。Soraprazan 与 H,K-ATPase 结合，Kd为 28.27 nM。Soraprazan 对酸分泌有直接抑制作用，对 H,K-ATPase 的选择性是 Na,K- 和 Ca- ATPases 的 2000 倍以上。

Soraprazan (BYK61359) is a selective, reversible K-competitive inhibitor of the H,K-ATPase (Ki=6.4 nM), with an IC50 of 0.19 μM in gastric glands. Soraprazan binds to the H,K-ATPase with a Kd of 28.27 nM.Soraprazan shows immediate inhibition of acid secretion and is more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases.

Soraprazan (BYK61359) is a potent inhibitor of gastric H,K-ATPase, with an IC50 of 0.1 μM when measured in ion-leaky vesicles in the presence of 1 mM potassium. Soraprazan (BYK61359) also effectively inhibits dibutyryl cAMP-stimulated [14C]AP accumulation in isolated gastric glands with an IC50 of 0.19 μM (0.09-0.40 μM geometric mean from n=6 with 95% confidence limits).

Soraprazan (1-27 μmol/kg; p.o.) shows rapid and consistent inhibition of acid secretion in dog .

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Others

Other Targets

Others

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261944-46-1

367.44

C21H25N3O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 200 mg/mL (544.31 mM; 超声助溶 )

COCCO[C@H]1[C@H](O)[C@H](Nc2c1ccn1c(C)c(C)nc21)c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years