Soraprazan (BYK61359) (Synonyms: BYK61359) |
カタログ番号GC30130 |
ソラプラザン (BYK61359) (BYK61359) は、胃腺で 0.19 μM の IC50 を持つ、H,K-ATPase (Ki=6.4 nM) の選択的可逆的 K 競合阻害剤です。
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Cas No.: 261944-46-1
Sample solution is provided at 25 µL, 10mM.
Soraprazan is a reversible, and fast-acting inhibitor of gastric H+/K+ ATPase.
Soraprazan 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 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). In ion-leaky vesicles, soraprazan is a potent k-competitive inhibitor of the H,K-ATPase, with Ki of 6.4 nM. Soraprazan binds to the H,K-ATPase in ion-leaky vesicles with a Kd of 26.4 nM and a Bmax of 2.89 nmol/mg[1].
[1]. Simon WA, et al. Soraprazan: setting new standards in inhibition of gastric acid secretion. J Pharmacol Exp Ther. 2007 Jun;321(3):866-74. Epub 2007 Mar 16.
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