| S8565 |
Omarigliptin (MK-3102) |
Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5). |
Selective |
DPP-4, IC50: 1.6 nM |
| S4636 |
Teneligliptin hydrobromide |
Teneligliptin (Teneligliptin hydrobromide anhydrous) 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. |
Selective |
DPP-4, IC50: 1.75 nM |
| S3033 |
Vildagliptin (LAF-237) |
Vildagliptin (LAF-237,NVP-LAF 237) inhibits DPP−4 with IC50 of 2.3 nM. |
Selective |
DPP-4, IC50: 2.3 nM |
| S5365 |
Alogliptin |
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. |
Selective |
DPP-4, IC50: 2.93 nM |
| S5909 |
Anagliptin |
Anagliptin is an orally active and highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor and exerts anti-inflammatory effects on macrophages, adipocytes, and mouse livers by suppressing NF-κB activation. |
Selective |
DPP-4, IC50: 3.3 nM |
| S7513 |
Trelagliptin |
Trelagliptin (SYR-472), a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM, improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM). |
Selective |
DPP-4, IC50: 4 nM |
| S5063 |
Trelagliptin succinate |
Trelagliptin succinate (SYR472) is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM). |
Selective |
DPP-4, IC50: 4 nM |
| S2868 |
Alogliptin (SYR-322) benzoate |
Alogliptin (SYR-322) benzoate 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. |
Selective |
DPP-4, IC50: <10 nM |
| S5079 |
Sitagliptin |
Sitagliptin (MK-0431) is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes. |
Selective |
DPP-4, IC50: 18 nM |
| S4002 |
Sitagliptin phosphate monohydrate |
Sitagliptin phosphate monohydrate (MK-0431) is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts. |
Selective |
DPP-4, IC50: 19 nM |
| S4697 |
Saxagliptin hydrate |
Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
Selective |
DPP-4, IC50: 26 nM |
| S1540 |
Saxagliptin (BMS-477118) |
Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
Selective |
DPP-4, IC50: 26 nM |
| S8455 |
Talabostat (PT-100) |
Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities. |
Pan |
DPP-4, IC50: <4 nM |
