A potassium-competitive acid blocker
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Revaprazan (hydrochloride)

Item No. 46259

Technical Information
Formal Name
4-(3,4-dihydro-1-methyl-2(1H)-isoquinolinyl)-N-(4- fluorophenyl)-5,6-dimethyl-2-pyrimidinamine, monohydrochloride
CAS Number
178307-42-1
Synonyms
  • SB-641257
  • YH 1885
Molecular Formula
C22H23FN4 • HCl
Formula Weight
Purity
≥98%
A solid
Acetonitrile:Water (1:1): Sparingly soluble: 1-10 mg/ml
SMILES
FC1=CC=C(NC2=NC(C)=C(C)C(N3CCC4=C(C3C)C=CC=C4)=N2)C=C1.Cl
InChi Code
InChI=1S/C22H23FN4.ClH/c1-14-15(2)24-22(25-19-10-8-18(23)9-11-19)26-21(14)27-13-12-17-6-4-5-7-20(17)16(27)3;/h4-11,16H,12-13H2,1-3H3,(H,24,25,26);1H
InChi Key
MALPZYQJEDBIAK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Revaprazan is a potassium-competitive acid blocker (P-CAB) that inhibits H+/K+-ATPase activity in porcine gastric mucosa membrane vesicles (IC50 = 0.35 µM).1 It rescues H. pylori-induced cytotoxicity and H. pylori-induced increases in prostaglandin E2 (PGE2; Item No. 14010) levels in AGS gastric epithelial cells, and it potentiates the antifungal activity of posaconazole (Item No. 14737) against Aspergillus in vitro.2,3 Revaprazan decreases disease severity in a rat model of indomethacin-induced intestinal damage.4 Formulations containing revaprazan have been used in the treatment of gastritis and gastric and duodenal ulcers.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yoon, Y.A., Park, C.S., Cha, M.H., et al. Novel pyrimidines as acid pump antagonists (APAs). Biooorg. Med. Chem. Lett. 20(19), 5735-5738 (2010).

    2. Lee, J.-S., Cho, J.-Y., Song, H., et al. Revaprazan, a novel acid pump antagonist, exerts anti-inflammatory action against Helicobacter pylori-induced COX-2 expression by inactivating Akt signaling. J. Clin. Biochem. Nutr. 51(2), 77-83 (2011).

    3. Cheng, W., Shen, M., Wan, L., et al. In vitro combination effects and mechanisms of Revaprazan with triazole antifungal drugs on Aspergillus. BMC Microbiol. 25(1), 715 (2025).

    4. Han, Y.M., Park, J.M., Her, S., et al. Revaprazan prevented indomethacin-induced intestinal damages by enhancing tight junction related mechanisms. Biochem. Pharmacol. 182, 114290 (2020).