gastric

Salsalate (Sasapyrine) is an orally available salicylate and non-steroidal anti-inflammatory drug (NSAID), with anti-inflammatory, analgesic and antipyretic activities.

Lansoprazole (A-65006) is a 2, 2, 2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Ranitidine Hydrochloride (AH19065) is a member of the class of histamine H2-receptor antagonists with antacid activity. Ranitidine is a competitive and reversible inhibitor of the action of histamine, released by enterochromaffin-like (ECL) cells, at the histamine H2-receptors on parietal cells in the stomach, thereby inhibiting the normal and meal-stimulated secretion of stomach acid. In addition, other substances that promote acid secretion have a reduced effect on parietal cells when the H2 receptors are blocked.

Proglumide (Binoside) is a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

Itopride hydrochloride (Ganaton) is an AChE and D2DR inhibitor.

Metyrosine (α-Methyltyrosine) is an antihypertensive drug and could be used as a tyrosine hydroxylase inhibitor.Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.

Ranitidine (HSDB 3925) is a non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.

Troxipide (Aplace), a new-type systemic non-antisecretory gastric cytoprotective agent, which is mucus-secreting, anti-ulcer, and anti-inflammatory properties irrespective of pH of stomach or duodenum.

HPi1 is a selective and orally active antimicrobial against Helicobacter pylori (IC50: 0.24 μM and a MIC of 0.08-0.16 μg/mL). HPi1 is inactive against other Xaliproden, including the gut commensals, Lactobacillus reuteri, Lactobacillus casei, and Bifidoba

Dimaprit dihydrochloride, a selective histamine H2 receptor agonist, inhibits nNOS with an IC50 of 49 μM and can stimulate gastric acid secretion.

Lafutidine (FRG-8813) is a newly developed histamine H2-receptor antagonist that inhibits gastric acid secretion.

Roxatidine Acetate hydrochloride (HOE 760) is a specific and competitive histamin H2-receptor antagonist. It inhibits gastric acid secretion and ulcer formation.

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM, effectively suppressing the proliferation of human gastric cancer cells by downregulating the PAK4/c-Src/EGFR/cyclin D1 pathway and inducing apoptosis.

Rabeprazole sodium (Habeprazole Sodium) is a 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of stomach ulcers and Zollinger-Ellison syndrome. The drug inhibits H(+)-K(+)-exchanging ATPase which is found in gastric parietal cells.

Tegoprazan is an orally active, highly selective gastric H+/K+-ATPase inhibitor that controls gastric acid secretion and motility, with an IC50 of 0.29-0.52 μM for porcine, canine, and human H+/K+-ATPase in vitro.

Ilaprazole sodium (IY-81149 sodium) , a substituted benzimidazole prodrug, is a selective and irreversible proton pump inhibitor. A weak base, Ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.

Ilaprazole (IY-81149) is a proton pump inhibitor used in the treatment of dyspepsia gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. Studies also showed that Ilaprazole significantly prevented the development of reflux oesophagitis.

MET Tyrosine Kinase Inhibitor PF-04217903 is an orally bioavailabe, small-molecule tyrosine kinase inhibitor with potential antineoplastic activity.

Irigenin mediates its antimetastatic effect by specifically and selectively blocking the α9β1 and α4β1 integrin binding sites on the C-C loop of the Extra Domain A domain. It can sensitize TRAIL-induced apoptosis by enhancing the expression of pro-apoptotic molecules in gastric cancer cells and has anti-cancer effects.

Solamargine (δ-Solanigrine) is a major steroidal alkaloid glycoside extracted from a traditional Chinese medicine herb, Solanum nigrum L. (SNL); has been shown to inhibit growth and induce apoptosis of various cancer cells.

Lentinan, isolated and purified from a hot water extract of Lentinula edodes fruit bodies, is a fungal polysaccharide immunomodulator with anti-tumor effects.

Tenatoprazole (TU-199), a prodrug of the proton pump inhibitor (PPI) class, can inhibit proton transport (IC50: 3.2 μM).

Xenopsin (Xenopsin(2TFA))(2TFA) is a neurotensin-like octapeptide previously isolated from amphibian skin.