dipeptidyl peptidase

Linagliptin (BI 1356) is a potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity.

Vildagliptin (LAF237) is a cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Vildagliptin's cyano moiety undergoes hydrolysis and this inactive metabolite is excreted mainly via the urine.

Trelagliptin succinate (SYR-472 succinate) is a long-acting inhibitor of dipeptidyl peptidase-4 (DPP-4), being developed for the treatment of type 2 diabetes (T2D).

Trelagliptin (SYR-472) is a highly specific, long-acting DPP-4 inhibitor.

Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus.

Retagliptin Phosphate (SP 2086) is pharmaceutical composition of DPP-4 inhibitor, for treating type-2 diabetes.

Puromycin aminonucleoside (NSC 3056) is an aminonucleoside antibiotic and a purine analog of puromycin. It can reversibly inhibit dipeptidyl peptidase and cytosolic alanine aminopeptidase, increase podocyte permeability by regulating ZO-1 in an oxidative stress-dependent manner, induce apoptosis, and promote the secretion of migrasomes. It is commonly used to induce nephrotic syndrome models in research.

Talabostat mesylate (PT100) is an orally active, selective inhibitor of dipeptidyl peptidases IV (DPP4, IC50: 0.18 nM), including tumor-associated fibroblast activation protein. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony-stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis.

UAMC00039 dihydrochloride is a potent, reversible, and competitive inhibitor of dipeptidyl peptidase II, with an IC50 of 0.48 nM.

Gemigliptin (LC15-0444) is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor(KD : 7.25 nM.)

Azaleatin is a natural product from Rhododendron simsii. Azaleatin is a dipeptidyl peptidase-IV inhibitor. Azaleatin can be used for type-2 diabetes and obesity studies.

Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively).

Dipeptidyl peptidase-IV (DPP-IV) is an enzyme that deactivates incretin hormones such as glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which are crucial in regulating blood glucose levels. Additionally, DPP-IV functions as a binding protein and ligand for various extracellular molecules. This enzyme is instrumental in research related to diabetes and cancer.

DPP-IV-IN-1 is an effective inhibitor of dipeptidyl peptidase IV (DPP-IV), a serine protease (IC50: 4.6 nM).

P32/98 hemifumarate is a dipeptidyl peptidase IV (DPP4) inhibitor with hypoglycemic properties that improves insulin sensitivity and β-cell responsiveness in the Zucker diabetic rat model, and may be useful in studies of type 2 diabetes and colitis.

Cameglipti, a dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type 2 diabetes.

Imigliptin (KBP 3853) is a novel dipeptidyl peptidase-4 inhibitor for the study of type 2 diabetes.

TS-021 is a selective dipeptidyl peptidase 4 (DPP-4) inhibitor with antidiabetic activity for the study of type 2 diabetes.

Leukotriene E4 (LTE4) (LTE4) is produced by the action of dipeptidyl peptidase on LTD4 and is a component of the Slow Reactive Substance of Anaphylaxis (SRS-A).LTE4 is present in plasma and urine and can be used to detect asthma.

Denagliptin is a small molecule dipeptidyl peptidase IV (DPP-4) inhibitor for the treatment of endocrine Ü metabolic diseases and can be used in the study of type 2 diabetes.

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent DPP-IV inhibitor with an IC50 of 19 nM in Caco-2 cell extracts.

Nateglinide (Senaglinide) is an oral hypoglycemic agent and amino acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Nateglinide has been linked to rare instances of clinically apparent acute liver injury.