Linagliptin (formerly known as BI-1356; trade names Tradjenta and Trajenta) is a xanthine-based, highly potent, selective, and competitive DPP-4 inhibitor with potential anti-diabetic activity.

Sitagliptin phosphate (formerly also known as MK-431; trade name Januvia; Xelevia; Janumet) monohydrate, the phosphate and hydrated form of Sitagliptin which is an antihyperglycemic agent and antidiabetic drug, is a potent, triazolopyrazine-based, and orally bioavailable inhibitor of DPP-IV (dipeptidyl peptidase-4) with IC50 of 19 nM in Caco-2 cell extracts.

Vildagliptin (formerly also known as NVP LAF237; DSP-7238; LAF-237; trade name: Zomelis) is an potent and orally bioavailable anti-diabetic drug that acts as an inhibitor of DPP-4 (dipeptidyl peptidase 4) with an IC50 of 2.3 nM.

Puromycin aminonucleoside (formerly known as NSC 3056; PAN, NSC-3056), the aminonucleoside portion of the antibiotic puromycin, is commonly used in nephrosis animal models as well as in the study of human glomerular disease, and glomerular function and morphology.

Alogliptin (formerly also known as SYR-322; trade names Nesina; Kazano, Oseni) is a novel, potent, orally bioavailable, and selective inhibitor of DPP-4 (serine protease dipeptidyl peptidase IV) with potential anti-hyperglycemic activity.

Alogliptin benzoate (SYR-322 benzoate; Nesina; Kazano, Oseni), the benzoate salt of alogliptin, is a novel, potent, orally bioavailable, and selective inhibitor of DPP-4 (serine protease dipeptidyl peptidase IV) with anti-diabetic effects.

Talabostat mesylate, the mesylate salt of Talabostat (PT-100; PT100 Val-boroPro), is an orally available inhibitor of dipeptidyl peptidase (DPP4, DPP8, and DPP9) with a Ki of 0.18 nM.

Teneligliptin HBr (formerly MP-513; MP513; trade name Tenelia in Japan), the hydrobromide salt of Teneligliptin, is a novel, potent, orally bioavailable and long-lasting dipeptidyl peptidase-4 (DPP-4) inhibitor; Teneligliptin is an approved drug for the treatment of type 2 diabetes mellitus in Japan.

Anagliptin (formerly known as SK0403) is a novel, potent, orally bioactive, highly selective inhibitor of DPP-4 (dipeptidyl peptidase 4) with an IC50 of 3.8 nM.

Saxagliptin hydrate (also known as BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate; brand name: Onglyza), the hydrate form of Saxagliptin, is a potent, orally bioactive, selective and reversible DPP4 (dipeptidyl peptidase-4) inhibitor with IC50 of 26 nM.