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Tegoprazan (CJ-12420, IN-A001, K-CAB, LXI-15028) is a potassium-competitive acid blocker and a potent, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro. Tegoprazan (3 μM) inhibits 86% of H+/K+-ATPase activity, whereas the inhibition is decreased to 34% after the dilution of Tegoprazan concentration to 0.15 μM.
In vivo, Tegoprazan (1.0 mg/kg, p.o.) potently and completely inhibits histamine-induced gastric acid secretion in dogs. Tegoprazan (1.0-3.0 mg/kg, p.o.) reverses the pentagastrin-induced acidified gastric pH to the neutral range.
| Molecular Weight | 387.38 |
| Formula | C20H19F2N3O3 |
| CAS Number | 942195-55-3 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ATPase Products |
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| Apoptolidin
Apoptolidin is a polyketide isolated from Nocardiopsis bacteria. |
| Transdermal Peptide Disulfide
Transdermal Peptide Disulfide (TD 1 Disulfide(peptide)) is a 11-amino acid peptide, binds toNa+/K+-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. |
| SPAI-1
SPAI-1 is a specific inhibitor for monovalent cation transporting ATPases. |
| Prilocaine acetate
Prilocaine acetate, an amino amide, is a Na/K-ATPase inhibitor. |
| Chamigrenol
Chamigrenol is a Na+/K+-ATPase inhibitor with an IC50 value of 15.9 μg/mL. |
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