Tegoprazan

SKU: orb1307685

Description

Tegoprazan is a potent and selective oral inhibitor of gastric H+/K+-ATPase, demonstrating in vitro IC50 values of 0.29-0.52 μM across species. It is utilized in research on gastric acid secretion, motility, and related gastrointestinal disorders, with applications in both in vitro enzymatic assays and in vivo pharmacological studies.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 942195-55-3
• MW: 387.38
• Purity: 98.22%
• Formula: C₂₀H₁₉F₂N₃O₃
• SMILES: CN(C)C(=O)c1cc(O[C@H]2CCOc3cc(F)cc(F)c23)c2[nH]c(C)nc2c1
• Target: Potassium Channel,ATPase,Proton pump
• Solubility: DMSO:22.5 mg/mL (58.08 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.16 mM)

Bioactivity

• Target IC50:
  H+, K+-ATPase:0.29-0.52 μM
• In Vivo:
  METHODS: Tegoprazan (CJ-12420) (3, 10 mg/kg, oral, 5 days) was used to treat pylorus-ligated rats, and the effects of Tegoprazan and esomeprazole on gastric acid secretion in pylorus-ligated rats were observed. RESULTS The gastric fundus pH values ​​of 3 mg/kg Tegoprazan were 4.13 and 4.34, respectively, and the gastric fundus pH values ​​of 10 mg/kg Tegoprazan were 6.86 and 6.63, respectively. Tegoprazan can completely inhibit gastric acid secretion.
• In Vitro:
  METHODS: BMM cells were cultured with Tegoprazan (CJ-12420) (0, 0.0005, 0.001, 0.005, 0.01, 0.05, 0.1, 0.5, 1, 10, 100 and 1000 μg/mL, 24 hours) to investigate its effects on BMM cytotoxicity and nitric oxide (NO) production. RESULTS When the concentration of Tegoprazan was 0.5, 1, 10 and 100 μg/mL, the cell viability exceeded 80%; when the concentration was 1000 μg/mL, the cell viability was less than 80%; 100 μg/mL of Tegoprazan could significantly inhibit NO production in BMM cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

acid, inhibit, Inhibitor, gastric, H+/K+-ATPase, secretion, pentagastrin, Tegoprazan, Proton Pump, Protonpump, Proton pump

Compound Identifiers

PubChem CID

23582846