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 |
| 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.
| Related ATPase Products |
|---|
| 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. |
| ZW290
ZW290 is a compound to activate brown adipose tissue (BAT) thermogenic function. |
| ATP synthase inhibitor 2 TFA
ATP synthase inhibitor 2 TFA is a Pseudomonas aeruginosa (PA) ATP synthase inhibitor (IC50=10 μg/mL). |
| Apicularen B
Apicularen B is a cytotoxic macrolide produced by Archangium gephyra and is also a specific V-ATPase inhibitor. Its IC50 values range from 0.2 to 1.2 μg/mL and it exhibits weak activity against some Gram-positive bacteria. |
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