Bioactivity | 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[1]. | ||||||||||||
Invitro | 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)[1]. | ||||||||||||
In Vivo | Soraprazan (1-27 μmol/kg; p.o.) shows rapid and consistent inhibition of acid secretion in dog [1]. | ||||||||||||
Name | Soraprazan | ||||||||||||
CAS | 261944-46-1 | ||||||||||||
Formula | C21H25N3O3 | ||||||||||||
Molar Mass | 367.44 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |