hydrolytic

KT203 is a selective and potent structural domain 6 (ABHD6) inhibitor of alpha/beta hydrolytic enzymes with potential antiviral and anti-inflammatory activity for the study of pneumonia.

Gabexate mesylate (FOY) is a serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

(3R,5R)-Rosuvastatin, a potential impurity detected in bulk rosuvastatin formulations, arises as a degradation product through various stresses including acid or base hydrolysis, thermal, photolytic, hydrolytic, oxidative stress, or during storage. This compound is associated with the HMG-CoA reductase inhibitor class to which rosuvastatin belongs.

N-Phthaloylglutamic acid is a hydrolytic metabolite of thalidomide.

PF04677490 is an effective PDE1 inhibitor. PF04677490 efficaciously inhibits cAMP- and cGMP-hydrolytic activity in preparations from human myocardium at concentrations selective for PDE1.

Orlistat degradation product is a degradation product of the digestive lipase inhibitor orlistat . It is formed via hydrolytic and thermal degradation as well as digestion by human carboxyl ester lipase.

Phenyl-glutarimide 4'-oxyacetic acid, a carboxylic acid-functionalized cerebellar ligand, is utilized in developing PROTAC deactivators due to its superior hydrolytic stability and efficacy. This compound exhibits enhanced binding to PROTAC, [1].

Arachidoyl ethanolamide, a saturated fatty acyl ethanolamide lacking classical (CB1/CB2) activity, plays a role in a complex system comprising central cannabinoid (CB1), peripheral cannabinoid (CB2), and non-CB receptor-mediated pharmacology. This system has paved the way for extensive research in diverse fields such as memory, weight loss and appetite, neurodegeneration, tumor surveillance, analgesia, and inflammation. Unlike other compounds, Arachidoyl ethanolamide does not bind to the murine CB1 receptor nor does it compete with anandamide for the fatty acid amide hydrolase, the endocannabinoid hydrolytic enzyme. The non-CB receptor-mediated actions of saturated ethanolamides like Arachidoyl ethanolamide are currently under investigation.

Phenyl-glutarimide 4'-piperazine, a piperazine-functionalized cereblon ligand, facilitates the development of PG-PROTACs with enhanced hydrolytic stability and potency compared to those produced with IMiD (immunomodulatory imide drug) analogs. It serves as a foundation for PROTACDegrader development.

Rebaudioside D is a potential sweetener. Rebaudioside D shows similar stability when exposed to simulate stomach and small intestine fluids, with susceptibility to hydrolytic degradation by enteric bacteria collected from the cecum.

Prostaglandin E1 (PGE1), synthesized through cyclooxygenase-mediated metabolism of dihomo-γ-linolenic acid (DGLA), functions by inhibiting platelet aggregation (IC50= 40 nM) and enhancing vasodilation. Its analog, 13,14-dihydro-16,16-difluoro PGE1, and the metabolite, 13,14-dihydro PGE1, both retain similar anti-aggregatory properties to the original compound. The inclusion of two electron-withdrawing fluorine atoms in 13,14-dihydro-16,16-difluoro PGE1 is believed to increase molecular stability and potentially extend bioavailability by resisting hydrolytic degradation.

Ancitabine hydrochloride (NSC 145668 HCl) is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine.

Naringinase is a hydrolytic enzymatic complex that exhibits α-L-rhamnosidase and β-D-glucosidase activities. It is widely found in nature and is primarily utilized for the biotransformation of steroids, antibiotics, and glycosides.

ERAP2-IN-1 (compound 61) is a non-competitive inhibitor of ERAP2. ERAP2-IN-1 specifically inhibits the hydrolytic activity of ERAP2 peptides, inhibiting Arg-AMC hydrolysis (IC50: 27 μM) and the hydrolytic activity of model peptides (IC50: 44 μM).