DPP-4
Dipeptidyl peptidase-4 (DPP-4), also known as CD26, is a membrane-associated and soluble serine exopeptidase that cleaves peptides containing alanine or proline at the penultimate N-terminal position, thereby regulating the biological activity of multiple peptide hormones and signaling molecules[1][2]. Mechanistically, DPP-4 is a key regulator of the incretin pathway because it rapidly degrades the active forms of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), generating truncated products with markedly reduced biological activity and limiting incretin-mediated glucose control[3][4][5]. Through this enzymatic process, DPP-4 influences insulin secretion, glucagon regulation, and systemic glucose homeostasis, making it a central component of metabolic signaling networks relevant to type 2 diabetes mellitus (T2DM) and related metabolic disorders[4][6][7]. In disease contexts, elevated DPP-4 activity has been associated with insulin resistance, inflammation, obesity, and T2DM, supporting its use as a mechanistic target and biomarker in metabolic research models[2]. Compared with related members of the dipeptidyl peptidase family, DPP-4 is distinguished by its well-characterized role in incretin degradation and its dual function as both an enzymatic regulator and a cell-surface signaling molecule, which contributes to its broad physiological relevance[1][2]. For experimental applications, selective DPP-4 inhibitors are widely used to prolong endogenous GLP-1 and GIP activity, enhance glucose-dependent insulin secretion, and improve glycemic control, providing robust pharmacological tools for investigating incretin biology and metabolic disease mechanisms[6][7][8].
References:
- [1]. Huang P K, Lin S R, Chang C H, et al. Natural phenolic compounds potentiate hypoglycemia via inhibition of Dipeptidyl peptidase IV[J]. Scientific Reports, 2019, 9(1): 15585.
- [2]. Pechmann LM, et al. The multiple actions of dipeptidyl peptidase 4 (DPP-4) and its pharmacological inhibition on bone metabolism: a review. Diabetol Metab Syndr. 2024 Jul 25;16(1):175. [Content Brief]
- [3]. Kieffer TJ, et al. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology. 1995 Aug;136(8):3585-96. [Content Brief]
- [4]. Müller TD, et al. Glucagon-like peptide 1 (GLP-1). Mol Metab. 2019 Dec;30:72-130. [Content Brief]
- [5]. Zheng Z, et al. Glucagon-like peptide-1 receptor: mechanisms and advances in therapy. Signal Transduct Target Ther. 2024 Sep 18;9(1):234. [Content Brief]
- [6]. Ahren B. DPP-4 inhibitors[J]. Best Practice & Research Clinical Endocrinology & Metabolism, 2007, 21(4): 517-533.
- [7]. Deacon C F. Peptide degradation and the role of DPP-4 inhibitors in the treatment of type 2 diabetes[J]. Peptides, 2018, 100: 150-157.
- [8]. Dalle S, Burcelin R, Gourdy P. Specific actions of GLP-1 receptor agonists and DPP4 inhibitors for the treatment of pancreatic 尾-cell impairments in type 2 diabetes[J]. Cellular signalling, 2013, 25(2): 570-579.
All Product Categories
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DPP-4 Related Products (110)
Related Products (110)
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TS-021 free base
0 ImagesSynonyms: DPP-IV-IN-1DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), a highly specific serine protease, with an IC50 of 4.6 nM.
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Gemigliptin
0 ImagesCat. No.: HY-14892CAS No.: 911637-19-9Synonyms: LC15-0444Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
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Vildagliptin dihydrate
0 ImagesCat. No.: HY-14291ACAS No.: 2133364-01-7Synonyms: LAF237 dihydrate; NVP-LAF 237 dihydrateVildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.
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Talabostat
0 ImagesCat. No.: HY-13233CAS No.: 149682-77-9Synonyms: Val-boroPro; PT100Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
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Fotagliptin
0 ImagesSynonyms: SAL067 free baseFotagliptin is a Dipeptidyl Peptidase IV (DPP-4) inhibitor (IC50=2.27 nM). Fotagliptin displays great security in rat and dog. Fotagliptin can be used for Type 2 diabetes mellitus research.
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Alogliptin-d3
0 ImagesSynonyms: SYR-322-d3 free baseAlogliptin-d3 is the deuterium labeled Alogliptin. Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes.
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NDMC101
0 ImagesNDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. 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.
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H-Glu(Met-OH)-OH
0 ImagesSynonyms: H-γ-Glu-Met-OH; γ-Glu-MetH-Glu(Met-OH)-OH (H-γ-Glu-Met-OH; γ-Glu-Met) is a DPP-IV inhibitor with an IC50 of 2.11 mM. H-Glu(Met-OH)-OH binds to DPP-IV’s active site to block substrate binding. H-Glu(Met-OH)-OH can be used for the research of type 2 diabetes.
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HAEGT
0 ImagesHAEGT is the first N-terminal 1-5 residues of glucagon like peptide-1 (GLP-1) peptide, and the sequence is His-Ala-Glu-Gly-Thr. HAEGT acts as a competitive substrate for probing prime substrate binding sites of human dipeptidyl peptidase-IV (DPP-IV) 1, in which the N-terminal His-Ala is catalyzed cleavage by DPP-IV. HAEGT can be used in the research of diabetes, obesity.
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Alogliptin-13C,d3
0 ImagesCat. No.: HY-A0023ASCAS No.: 1246817-18-4Synonyms: SYR-322-13C,d3Alogliptin-13C,d3 is the deuterium labeled Alogliptin. Alogliptin is a potent and selective inhibitor of DPP-4.
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PK44 phosphate
0 ImagesCat. No.: HY-110083CAS No.: 1017682-66-4PK44 phosphate is a potent dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 value of 15.8 nM.
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Teneligliptin-d8
0 ImagesCat. No.: HY-14806SCAS No.: 1391012-95-5Synonyms: MP-513 d8Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor.
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Nateglinide-d5
0 ImagesSynonyms: A4166 d5; Senaglinide d5Nateglinide-d5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].
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DBPR108
0 ImagesDBPR108 is an orally active, selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 of 15 nM. DBPR108 reduces glycated hemoglobin, fasting plasma glucose and postprandial plasma glucose levels, increases serum active GLP-1 and insulin levels, and improves glucose tolerance. DBPR108 can be used in research related to type 2 diabetes.
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Prodipine hydrochloride
0 ImagesProdipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
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VAMP
0 ImagesVAMP, a tetrapeptide, is a competitive dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 1.00 μM and a Kd of 6.89 μM. VAMP effectively targets the DPP-IV-GLP-1 axis and can be used for the study of type 2 diabetes.
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Zomepirac acyl-O-β-D-glucuronide
0 ImagesCat. No.: HY-W121887CAS No.: 75871-31-7Synonyms: Zomepirac glucuronideZomepirac acyl-O-β-D-glucuronide (Zomepirac glucuronide) is a dipeptidyl peptidase IV Inhibitor. Zomepirac acyl-O-β-D-glucuronide is an unstable and chemically reactive metabolite of Zomepirac (HY-B0890A). Zomepirac acyl-O-β-D-glucuronide forms covalent adducts with cell membrane glycoproteins. Zomepirac acyl-O-β-D-glucuronide can be used for research on immunotoxicity.
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Anagliptin hydrochloride
0 ImagesCat. No.: HY-14877ACAS No.: 1359670-56-6Synonyms: SK-0403 hydrochlorideAnagliptin (SK-0403) hydrochloride is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.
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DPP-4-IN-18
0 ImagesCat. No.: HY-Z1764CAS No.: 486460-31-5Synonyms: Sitagliptin impurity 3DPP-4-IN-18 (Sitagliptin impurity 3) (Compound 4) impurity 3 is a potent, selective and orally active DPP-4 inhibitor with an IC50 of 27 nM. DPP-4-IN-18 can effectively prevent DPP-4 from degrading glucagon-like peptide 1 (GLP-1), thereby increasing the level of active GLP-1. DPP-4-IN-18 can be used for the research of type 2 diabetes.
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(S)-Sitagliptin phosphate
0 ImagesCat. No.: HY-13749CCAS No.: 823817-58-9Synonyms: (S)-MK-0431 phosphate(S)-Sitagliptin phosphate ((S)-MK-0431 phosphate) is the S-isomer of Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate (MK-0431 phosphate) is a potent DPP4 inhibitor. (S)-Sitagliptin phosphate can be used in diabetes research.
