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

Sitagliptin phosphate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.

Talabostat mesilate is an orally active, specific inhibitor of dipeptidyl peptidases with IC50 of 1 nM for DPP4, including tumor-associated fibroblast activation protein.

5-O-Demethylnobiletin, a flavonoid isolated from the peel of Citrus nobilis Lour., shows a certain inhibitory effect on DPP-IV enzyme.

Saxagliptin, the monohydrate form of anhydrous saxagliptin, is a reversible and selective DPP4 inhibitor with IC50 of 26 nM. It is used for the treatment of type 2 diabetes.

Metabolic Disease

Boc-3-hydroxy-1-adamantyl-D-glycine is used in the preparation of a Saxagliptin intermediate.

DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM showing no inhibition on DDP8 and DPP9.

Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM) and > 10 fold less potent for DPP-8 and DPP-9.

Alogliptin benzoate is the benzoate salt form of alogliptin which is a selective inhibitor of DPP-4 with IC50 of 6.9 nM that exhibits greater selective than DPP-2, DPP-8 and DPP-9.

Saxagliptin, also known as BMS-477118, is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Saxagliptin was approved in 2008 for the treatment of type 2 diabetes. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. .

Sitagliptin is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.

Omarigliptin, also called MA-3102, is an selective inhibitor of DPP-4 with IC50 of 1.6 nM and Ki of 0.8 nM. Its selectivity is higher than other 168 proteasomes.

Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

Diprotin A is the inhibitor of dipeptidyl peptidase IV. It can inhibit entry of HIV-1 or HIV-2 into T lymphoblastoid and monocytoid cell lines.

NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene express. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al .

Saikogenin A, extracted from a Chinese herbal plant called Tsai-Fu, is a dipeptidyl peptidase-IV (DPP-IV) inhibitor.