1. Membrane Transporter/Ion Channel
  2. Proton Pump Na+/K+ ATPase
  3. Tegoprazan-d6

Tegoprazan-d6  (Synonyms: CJ-12420-d6; RQ-00000004-d6)

Cat. No.: HY-17623S
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Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, 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 significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases.

For research use only. We do not sell to patients.

Tegoprazan-d<sub>6</sub> Chemical Structure

Tegoprazan-d6 Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, 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 significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases[1][2][3].

In Vitro

Tegoprazan (1.0 mM and 3.0 mM, 4 h) reduces DSS-induced colitis by maintaining high junction integrity of the epithelial mucosa in Caco-2 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: Caco-2 cells
Concentration: 1.0 mM and 3.0 mM
Incubation Time: 4 h
Result: Protected the intestinal epithelial tight junction barrier and inhibits the increase in intestinal permeability.
In Vivo

Tegoprazan (30 mg / kg, p.o., twice daily for 5 days) alleviates the severity of dinitrobenzene sulfonic acid (DNBS)-induced reduced colon length and colonic damage, as well as protecting against DNBS-induced colon inflammation in mice colon[1].
Tegoprazan (3 mg/kg and 10 mg/kg, p.o., 5 h) inhibits basal gastric acid secretion in a dose-dependent manner[2].
Tegoprazan (0.1, 1 and 10 mg/kg, p.o.) exerts an antiulcer effect in a dose-dependent manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pylorus-Ligated Rats[2]
Dosage: 3 mg/kg and 10 mg/kg
Administration: p.o., a single dose
Result: Inhibited basal gastric acid secretion in a dose-dependent manner and was effective at a single dose in Pylorus-Ligated rats.
Animal Model: Naproxen-induced acute gastric ulcer rat model[2]
Dosage: 0.1, 1 and 10 mg/kg
Administration: p.o., a single day or daily for 5 days
Result: Exerted an antiulcer effect in a dose-dependent manner and was effective at a single dose in naproxen-induced acute gastric ulcer rat model.
Animal Model: DNBS and Tegoprazan-induced rats[2]
Dosage: 30 mg/kg
Administration: p.o., twice daily for 5 days
Result: Reduced mRNA expression levels of proinflammatory cytokines, especially interleukin-17 (IL17) in DNBS and Tegoprazan-induced rats.
Molecular Weight

393.42

Formula

C20H13D6F2N3O3

Unlabeled CAS

942195-55-3

SMILES

CC1=NC2=C(C=C(C=C2N1)C(N(C([2H])([2H])[2H])C([2H])([2H])[2H])=O)O[C@H]3CCOC4=C3C(F)=CC(F)=C4

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tegoprazan-d6
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HY-17623S
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