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    • 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)pheny...

    2026-01-15

    3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide: Precision H+,K+-ATPase Inhibition for Gastric Acid Secretion Research

    Executive Summary: 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide (SKU: A2845) is a high-purity, potent H+,K+-ATPase inhibitor for research on gastric acid secretion and antiulcer mechanisms (APExBIO). It demonstrates an IC50 of 5.8 μM for H+,K+-ATPase and 0.16 μM for histamine-induced acid formation, making it significantly more potent than conventional tools. Its solubility in DMSO (≥17.27 mg/mL) and chemical stability at -20°C enable reproducible experimental workflows. The compound is supplied at ≥98% purity, verified by HPLC and NMR. Its validated profile underpins reliable in vitro and in vivo models of gastric acid-related disorders (Kong et al., 2025).

    Biological Rationale

    Gastric acid secretion is a fundamental physiological process regulated by the gastric H+,K+-ATPase, also known as the proton pump. Dysregulation of this process underlies peptic ulcer disease, gastroesophageal reflux disease, and other acid-related disorders (Kong et al., 2025). Inhibition of H+,K+-ATPase leads to a reduction in gastric acid output, providing a mechanistic basis for antiulcer therapy. Animal models employing H+,K+-ATPase inhibitors are critical for dissecting the pathways involved in acid secretion and mucosal protection, and for testing the efficacy of candidate antiulcer agents (applied use case—this article extends the comparison with IC omeprazole analogs by focusing on purity and solubility parameters).

    Mechanism of Action of 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide

    3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide acts as a selective and reversible inhibitor of the gastric H+,K+-ATPase enzyme. It binds to the catalytic site of the enzyme, blocking the translocation of protons into the gastric lumen. This inhibition disrupts the final step in acid secretion, resulting in a marked decrease in gastric acidity (next-generation review—this article adds quantitative IC50 data and workflow parameters). The compound exhibits an IC50 of 5.8 μM for H+,K+-ATPase and 0.16 μM for histamine-stimulated acid formation in isolated gastric glands (37°C, pH 7.4, 30 min incubation) (APExBIO).

    Evidence & Benchmarks

    • Demonstrates high-potency H+,K+-ATPase inhibition with an IC50 of 5.8 μM in enzyme assays (37°C, pH 7.4) (APExBIO Product Page).
    • Shows robust inhibition of histamine-induced gastric acid formation with an IC50 of 0.16 μM in isolated glandular preparations (APExBIO).
    • Supplied at ≥98% purity by HPLC and NMR, ensuring reproducibility for in vitro and in vivo studies (APExBIO).
    • Solubility in DMSO is ≥17.27 mg/mL, supporting high-concentration stock solutions. Compound is insoluble in water and ethanol (APExBIO).
    • Validated as a standard for peptic ulcer disease models, outperforming several IC omeprazole analogs in potency and selectivity (internal dossier—this article details updated validation and purity metrics).
    • Used in emerging research to model the impact of gastric acid modulation on the gut-brain axis and neuroinflammation (Kong et al., 2025).

    Applications, Limits & Misconceptions

    This compound is primarily used for:

    • Modeling gastric acid secretion and inhibition in cell-based and animal studies.
    • Benchmarking antiulcer activity in preclinical workflows.
    • Investigating the proton pump inhibition pathway in gastric mucosal protection.
    • Exploring the interaction between acid suppression and systemic processes, including neuroinflammatory signals (Kong et al., 2025).

    It is not indicated for diagnostic or clinical use. The compound’s insolubility in water and ethanol necessitates DMSO as a solvent. Long-term solution storage is not recommended due to decreased stability; instead, aliquots should be freshly prepared from powder for each experiment. For detailed best practices, see the 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide product page.

    Common Pitfalls or Misconceptions

    • Misconception: Compound can be used in clinical or diagnostic settings.
      Fact: It is for research use only (APExBIO).
    • Misconception: Compound is soluble in aqueous buffers or ethanol.
      Fact: Only soluble in DMSO at ≥17.27 mg/mL.
    • Misconception: Stable for long-term storage in solution.
      Fact: Stability is optimal at -20°C as a solid; solutions should be freshly prepared.
    • Misconception: All H+,K+-ATPase inhibitors perform identically.
      Fact: This compound exhibits greater potency and selectivity than many IC omeprazole analogs.
    • Misconception: Suitable for in vivo use without solubility or vehicle optimization.
      Fact: DMSO-based stock solutions require careful dilution protocols.

    Workflow Integration & Parameters

    For laboratory workflows, reconstitute the solid in DMSO at a minimum concentration of 17.27 mg/mL. Avoid aqueous or alcoholic solvents. Store powder at -20°C, protected from light and moisture. Prepare fresh aliquots before use to ensure activity. For in vitro assays, standard incubation conditions are 37°C, pH 7.4, with 30 min pre-incubation for enzyme and cell-based studies. In vivo protocols must optimize vehicle composition and dosing schedules for solubility and bioavailability (internal article—this article updates workflow recommendations for advanced reproducibility).

    Researchers modeling peptic ulcer disease or testing novel antiulcer agents should use this compound as a positive control or mechanistic probe. For multidimensional studies intersecting acid secretion and gut-brain axis research, its validated inhibition profile supports high-fidelity translational models (mechanism review).

    Conclusion & Outlook

    3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide is a gold-standard H+,K+-ATPase inhibitor for gastric acid secretion research. Its precise IC50 values, exceptional purity, and optimized solubility parameters enable robust modeling of acid-related disorders and antiulcer activity. As research expands into gut-liver-brain interactions and neuroinflammation, this compound's reliability and validation profile will remain pivotal for both mechanistic and translational investigations (Kong et al., 2025). For authoritative sourcing and technical documentation, refer to the APExBIO product page.