DPP-4

Omarigliptin (MK-3102) has been used in trials studying the treatment of Type 2 Diabetes Mellitus and Chronic Renal Insufficiency.

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.

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.

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

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.

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.

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).

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 phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.

Alogliptin Benzoate (SYR 322)(SYR 322), an effective and specific DPP-4 inhibitor (IC50<10 nM), exhibits greater than 10, 000-fold selectivity over DPP-8 9. Alogliptin may inhibit inflammatory responses by preventing the toll-like receptor 4 (TLR-4)-mediated formation of proinflammatory cytokines.

Anagliptin (SK-0403) is a potent Inhibitor of DPP-4(IC50 of 3.8 nM), for the treatment of type 2 diabetes mellitus.

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

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

Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation. Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity.

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

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

Saxagliptin (BMS-477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

Diprotin A (Ile-Pro-Ile) (Ile-Pro-Ile) is a dipeptidyl peptidase IV (DPP-IV) inhibitor.

DBPR108 is an orally bioavailable dipeptide-derived DPP4 inhibitor (IC50: 15 nM) and it has no inhibition on DDP8 and DPP9.

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

Gemigliptin Tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive inhibitor of dipeptidyl peptidase-4 (DPP-4). It has an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties.

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.

Teneligliptin hydrobromide (MP-513 (hydrobromide)) is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

Alogliptin (SYR-322)(SYR-322) is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10, 000-fold selectivity over DPP-8 and DPP-9.

Picolamine acts as a potential inhibitor of DPP-4.

3-Pyridylacetic acid hydrochloride (3-PAA-HCl) is a high homologue of niacin. It is a decomposition product of nicotine (and other tobacco alkaloids). It can also react with amines, alcohols and carboxylic acids, and can also act as an acid in the reaction. catalyst.

DPP-IV-IN-2 (H-Lys(4-nitro-Z)-pyrrolidide) is an inhibitor of both DP8/9 and dipeptidyl peptidase IV (IC50s: 0.1 and 0.95 μM).

Saikogenin A is a dipeptidyl peptidase-4 inhibitor.