secretory

Tris(2,4-di-tert-butylphenyl)phosphate (TDTBPP) isolated from Vitex negundoL inhibits secretory phospholipase A2 (sPLA2). Tris(2,4-di-tert-butylphenyl)phosphate has anti-inflammatory activity.

Varespladib (LY315920), a specific and effective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor(IC50=7 nM), has been investigated for the treatment and prevention of sickle cell disease, vaso-occlusive crisis, and acute coronary syndrome.

PD 128042 (CI 976) is a potent, orally active, and selective ACAT inhibitor (IC50: 73 nM) as well as a lysophospholipid acyltransferase (LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps.

Betazole dihydrochloride (Betazole hydrochloride) is an agonist of H2 receptor.

BTM-1086 is a potent gastric secretory inhibitor and an anti-ulcer agent.

Varespladib methyl (LY333013), a bioavailable prodrug of Varespladib, is a selective group II secretory phospholipase A2 inhibitor.

Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) is a proton pump inhibitor drug, used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.

Diphenmanil methylsulfate (Diphemanil mesylate), a quaternary ammonium anticholinergic, binds muscarinic acetylcholine receptors and thus decreases secretory excretion of stomach acids, sweat, and saliva.

Pantoprazole (BY1023) is a proton pump inhibitor used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.

Pantoprazole sodium (Pantecta) is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole sodium is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+/K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.

KU14R is a novel I(3)-R antagonist that selectively inhibits the insulin secretory response to imidazolines.

SCH28080 is a reversible and K+-competitive inhibitor of gastric H+/K+-ATPase with an IC50 value of 20 nM (rabbit microsomal membrane).SCH28080 is a potent inhibitor of acid secretion in vivo with anti-ulcer activity, anti-secretory and cytoprotective activity.

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.

GK241 (compound 31a-c), a 2-oxoamide-based compound, exhibits inhibitory activity against group IIA secretory phospholipase A2 (GIIA sPLA2) in humans and mice, with IC50 values of 143 nM and 68 nM, respectively. The mechanism of inhibition has been explored through molecular dynamics simulations.

Cholylsarcosine is a synthetic, non-secretory, and binding-resistant conjugated bile acid analog used in the treatment of fat malabsorption caused by severe bile acid malabsorption.

Brovanexine is known for its expectorant properties, selectively enhancing secretions from SG and dissolving acidic glycoproteins within secretory cell granules.

Diallylmelamine is an anti-secretory agent for the stomach.

BML-265 is a potent inhibitor of EGFR tyrosine kinase (EGFR tyrosine kinase). It disrupts Golgi apparatus integrity in human cells and hinders the transport of secretory proteins across various substances. In contrast, BML-265 does not affect the integrity and transport of the Golgi apparatus in rodent cells.

Ro 23-9358 is a potent inhibitor of secretory phospholipase A2, exhibiting anti-inflammatory properties.

Trimegestone, a highly effective oral progestogen, is used for endometrial protection, all doses inducing secretory endometrial transformation.

Namptactivator-5 (compound C8) is a potent activator of nicotinamide phosphoribosyltransferase (NAMPT), with a KD value of 6.19 µM. This compound demonstrates cellular anti-aging effects by promoting NAD+ production in the brain and reducing markers and secretory phenotypes associated with aging. Namptactivator-5 holds potential for researching age-related diseases.

Glutaminyl Cyclase Inhibitor 6 (compound BI-43) functions as an inhibitor of both secretory glutaminyl cyclase (sQC) and golgi-resident glutaminyl cyclase (gQC), with IC50 values of 0.012 µM and 0.040 µM, respectively. This compound also holds potential for research in Parkinson's disease.

Competitive inhibitor of secretory phospholipase A2 (sPLA2)

IOWH-032 (IOWH032) , a synthetic CFTR inhibitor, has been investigated for the treatment of cholera, diarrhea, and secretory diarrhea.