DPP-4

Choose Selective DPP-4 Inhibitors

DPP-4 Signaling Pathway Map

DPP-4 Signaling Pathways

DPP-4 Products

  • All (15)
  • DPP-4 Inhibitors (15)
  • New DPP-4 Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0122New Gemigliptin

Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.

S1540 Saxagliptin (BMS-477118) Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Turk J Pharm Sci, 2019, 16(2):227-233
Cancer Cell, 2018, 34(4):659-673
J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257
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.
Cell Rep, 2017, 20(7):1692-1704
S3031 Linagliptin (BI-1356) Linagliptin (BI-1356) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S3033 Vildagliptin (LAF-237) Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.
J Biol Chem, 2020, jbc.RA120.014831
Brain Res Bull, 2019, 147:78-85
Cell Rep, 2017, 20(7):1692-1704
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.
J Biomol Struct Dyn, 2021, 1-12
J Diabetes Res, 2020, 2020:2450781
Circulation, 2017, 135(20):1935-1950
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.
S4697 Saxagliptin hydrate Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Turk J Pharm Sci, 2019, 16(2):227-233
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).
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.
Med Sci Monit, 2021, 27:e928933
J Biol Chem, 2020, 10.1074/jbc.RA119.010894
J Diabetes Res, 2020, 2020:2450781
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.
Sci Adv, 2021, 7(27)eabh3032
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.
S7513 Trelagliptin Trelagliptin (SYR-472) is a highly selective, long-acting DPP-4 inhibitor. Phase 3.
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.
Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.08.015
J Invest Dermatol, 2019, S0022-202X(19)33499-2
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).
Acta Pharmacol Sin, 2021, 1-9
Front Behav Neurosci, 2021, 15:705579
E0122New Gemigliptin

Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.

S1540 Saxagliptin (BMS-477118) Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Turk J Pharm Sci, 2019, 16(2):227-233
Cancer Cell, 2018, 34(4):659-673
J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257
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.
Cell Rep, 2017, 20(7):1692-1704
S3031 Linagliptin (BI-1356) Linagliptin (BI-1356) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S3033 Vildagliptin (LAF-237) Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.
J Biol Chem, 2020, jbc.RA120.014831
Brain Res Bull, 2019, 147:78-85
Cell Rep, 2017, 20(7):1692-1704
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.
J Biomol Struct Dyn, 2021, 1-12
J Diabetes Res, 2020, 2020:2450781
Circulation, 2017, 135(20):1935-1950
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.
S4697 Saxagliptin hydrate Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Turk J Pharm Sci, 2019, 16(2):227-233
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).
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.
Med Sci Monit, 2021, 27:e928933
J Biol Chem, 2020, 10.1074/jbc.RA119.010894
J Diabetes Res, 2020, 2020:2450781
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.
Sci Adv, 2021, 7(27)eabh3032
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.
S7513 Trelagliptin Trelagliptin (SYR-472) is a highly selective, long-acting DPP-4 inhibitor. Phase 3.
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.
Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.08.015
J Invest Dermatol, 2019, S0022-202X(19)33499-2
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).
Acta Pharmacol Sin, 2021, 1-9
Front Behav Neurosci, 2021, 15:705579
E0122New Gemigliptin

Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.

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