pepsin

Pepsin is an endopeptidase that breaks down proteins into smaller peptides and amino acids that can be easily absorbed in the small intestine[1]. Pepsin is stable at pH ranges as high as pH 6. Above this pH, pepsin is rapidly irreversibly inactivated and elevation of pH of the reaction mixture to pH 8 results in complete inactivation of pepsin[2]. Pepsin has been posited to be a reliable biological marker of EER. An immunologic pepsin assay of combined sputum and saliva was determined to be 100% sensitive and 89% specific for detection of EER (based on pH-metry), and an enzymatic test of nasal lavage fluid (100% sensitivity and 92.5% specificity) demonstrated an increased incidence of EER in patients with chronic rhinosinusitis[3]. Cultured hypopharyngeal epithelial (FaDu) cells were exposed to human pepsin (0.1 mg mL) at pH 7.4 for either 1 hour or 12 hours at 37°C and both mitochondria and Golgi complexes were clearly damaged. This finding reveals a novel mechanism by which pepsin could cause cell damage, potentially even in nonacidic refluxate[4].

Pepsin A, a primary gastric protease in both pigs and humans, functions similarly to minor gastric proteolytic enzymes. It plays a crucial role in the proteolysis of food proteins within the vertebrate stomach [1] [2].

Pepsinostreptin is a pepsin inhibitor that forms a 1:1 complex with pepsin and suppresses its activity.

Aspergillopepsin I (Aspergillus acid protease) is an aspartic endopeptidase that catalyzes peptide bond hydrolysis within proteins, exhibiting broad specificity [1].

Cimetidine (SKF-92334) is a histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.

Pepstatin (Pepsin Inhibitor S 735A) is an aspartate protease inhibitor that also inhibits HIV protease activity with specific and oral activity. Pepstatin inhibits autophagy.

Pepstatin Trifluoroacetate (Pepstatin A), a specific and orally active aspartic protease inhibitor produced by actinomycetes, demonstrates inhibition efficacy with IC50 values of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM, and 260 nM against hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease, and hemoglobin-acid protease, respectively. Additionally, it effectively inhibits HIV protease.

NB-360 is a potent and brain-penetrable inhibitor of BACE1 and BACE2 with IC50s of 5, 5, and 6 nM for mouse and human BACE1 and BACE2. NB-360 exhibits excellent selectivity over the related aspartyl proteases pepsin, cathepsin E, and cathepsin D.

Pepstatin Ammonium is a specific inhibitor of aspartic proteaseproduced by actinomycetes(hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM

Statine is a protease inhibitor that is active against pepsin and other acid proteases.

Sucralfate (Sucrose octasulfate–aluminum complex) is a cytoprotective agent, an oral gastrointestinal medication primarily indicated for the treatment of active duodenal ulcers.

Imarikiren (also known as TAK-272) is a potent, highly selective, orally bioavailable direct renin inhibitor primarily used for treating diabetic nephropathy. In hPRA assays, TAK-272 exhibits strong inhibitory activity against human renin (IC50 = 2.1 nM) and demonstrates excellent selectivity over other aspartic proteases such as pepsin (IC50 > 10 μM) and cathepsin D (IC50 > 10 μM). In rats, TAK-272 shows significantly improved pharmacokinetic properties (F = 25.2%) and, upon oral administration (3 and 10 mg kg), exhibits a dose-dependent, potent, and sustained antihypertensive effect. Currently, TAK-272 HCl is undergoing human clinical trials.

H 256 is a pepsin heptapeptide inhibitor.

Streptomyces pepsin inhibitor is used as a pepsin inhibitor.

LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including pepsin, cathepsin D, or renin.

Sucralfate is a gastrointestinal protectant that includes sucrose octasulfate . Sucralfate protects gastric epithelial cells against acid- and pepsin-induced damage. Sucrose hexasulfate is a polysulfated disaccharide that is used as a reference standard for sucralfate.

Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.

Polignate Sodium is an Enzyme Inhibitor (Pepsin)

Rennin (Chymosin) is a proteolytic enzyme related to pepsin, produced in the stomachs of certain animals, that effectively coagulates liquid milk into a semi-solid form, prolonging its retention in the stomach. It specifically targets K-casein, cleaving the peptide bond between the amino acid residues phenylalanine and methionine (105 and 106), and plays a crucial role in cheese production [1].

H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that serves as a substrate for the enzymes cathepsin D, pepsin, and pepsinogen, with potential applications in biochemical analysis [1] [2].

Gastric inhibitory peptide (GIP) (1-42), an endogenous incretin hormone comprising 42 amino acids, promotes insulin secretion. Expressed in the intestinal neuroendocrine K cells and submandibular gland, it enters circulation after meals. GIP (1-42) blocks histamine, pentagastrin, and insulin-induced gastric acid and pepsin secretion, enhances glucose-stimulated insulin release, and accelerates gastric emptying in rats.

1. Dehydroabietic acid (Dehydroabietate) (DAA) is an EBV-EA activation inhibitor. 2. DAA is a useful food-derived compound for treating obesity-related diseases, by decreasing plasma glucose, insulin levels, plasma triglyceride (TG) , and hepatic TG levels. 3. DAA derivatives displays anti-secretory and anti-pepsin effect in animal models.

L-Lysine-13C6-15N2 Hydrochloride is L-Lysine hydrochloride labeled with 13C and 15N isotopes. L-Lysine hydrochloride is an essential amino acid for humans and a common food additive. It stimulates the secretion of pepsin and gastric acid, enhances gastric juice secretion, and promotes growth and development in children.

Kinetensin acetate(103131-69-7 free base) is isolated from pepsin-treated human plasma. Kinetensin acetate(103131-69-7 free base) is a neurotensin-like peptide.