| S5079 |
Sitagliptin
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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.
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Small Sci, 2025, 5(12):e202500140
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Pharmacol Res, 2025, 215:107696
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Sci Rep, 2025, 15(1):30226
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| S3033 |
Vildagliptin
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Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM.
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Int J Mol Sci, 2024, 25(18)9760
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J Clin Invest, 2023, 133(12)e165933
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Oncoimmunology, 2023, 12(1):2268257
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| S4002 |
Sitagliptin phosphate monohydrate
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Sitagliptin phosphate monohydrate (MK-0431) is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts.
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Small Sci, 2025, 5(12):e202500140
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J Cell Mol Med, 2025, 29(11):e70581
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Front Oncol, 2021, 11:704024
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| S1540 |
Saxagliptin (BMS-477118)
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Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with an IC50 of 26 nM.
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Turk J Pharm Sci, 2019, 16(2):227-233
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Cancer Cell, 2018, 34(4):659-673
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J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257
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| S8455 |
Talabostat (Val-boroPro, PT-100) Mesylate
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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.
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Int J Mol Sci, 2025, 26(5)2237
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J Oral Microbiol, 2024, 16(1):2373040
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Brain Res, 2024, S0006-8993(24)00383-4
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| S8565 |
Omarigliptin (MK-3102)
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A competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM), Omarigliptin (MK-3102) 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).
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NYMC Student Theses and Dissertations, 2023,
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Acta Pharmacol Sin, 2021, 1-9
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Front Behav Neurosci, 2021, 15:705579
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| S2868 |
Alogliptin (SYR-322) benzoate
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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.
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Cell Rep, 2017, 20(7):1692-1704
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| S5365 |
Alogliptin
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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.
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Sci Adv, 2021, 7(27)eabh3032
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| S4697 |
Saxagliptin hydrate
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Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
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Turk J Pharm Sci, 2019, 16(2):227-233
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| E3049 |
Lobeliae Chinensis Extract
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Lobeliae Chinensis Extract is extracted from Lobeliae Chinensis, which is a traditional Chinese herb widely used in the treatment of diabetes and found to have a hypoglycaemic mechanism related to the inhibition of DPP4.
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