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.
| Molecular Weight | 367.44 |
| CAS Number | 261944-46-1 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[4] Nisha Devi, et al. Medicinal Attributes of Imidazo[1,2-a]pyridine Derivatives: An Update
[5] W A Simon, et al. Soraprazan: setting new standards in inhibition of gastric acid secretion
| Related Proton Pump Products |
|---|
| Caloxin 2A1
Caloxin 2A1 is an extracellular plasma membrane Ca2+-ATPase (PMCA) peptide inhibitor. |
| CS-526
CS-526 is a potent, selective, reversible and orally active acid pump antagonist. |
| Revaprazan
Revaprazan (SB 641257) is a reversible proton pump inhibitor with significant anti-inflammatory effects. Revaprazan can be used for chronic gastric inflammation research. |
| Vonoprazan hydrochloride
Vonoprazan hydrochloride, a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan hydrochloride inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. |
| Abeprazan hydrochloride
Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H+, K+- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases. |
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