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 (102)
Related Products (102)
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Sitagliptin
0 ImagesSynonyms: MK-0431Sitagliptin (MK-0431) is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
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Talabostat mesylate
0 ImagesSynonyms: Val-boroPro mesylate; PT100 mesylateTalabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the 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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Diprotin A
0 ImagesSynonyms: Ile-Pro-IleDiprotin A (Ile-Pro-Ile) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
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Sitagliptin phosphate
0 ImagesSynonyms: MK-0431 phosphateSitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
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HBK001
0 ImagesCat. No.: HY-182580CAS No.: 1942922-78-2HBK001 is an orally active and selective dual GPR119 agonist and DPP-IV inhibitor. HBK001 triggers cAMP production, PKA activation, CREB phosphorylation, glucose-stimulated insulin secretion, plasma incretin elevation, β-cell proliferation, and β-cell function gene up-regulation. HBK001 reduces blood glucose, ameliorates hyperglycemia, improves glucose tolerance, and enhances islet morphology. HBK001 can be used for the research of type 2 diabetes mellitus.
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DeDPP4
0 ImagesCat. No.: HY-182336DeDPP4 is a DPP-4 PROTAC degrader. DeDPP4 induces sustained elevation of glucagon-like peptide-1 (GLP-1), enhances glucose tolerance, causes persistent reduction of blood glucose, and achieves long-term blood glucose regulation in animal models of type 2 diabetes. DeDPP4 mediates dose-dependent DPP-4 depletion in cancer cells, and also targets and degrades DPP-4 in the liver and adipose tissues of animal models with type 2 diabetes. DeDPP4 can be used for the research of type 2 diabetes and non-small cell lung cancer.
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Cyclocarin A
0 ImagesCat. No.: HY-N17777CAS No.: 1403937-45-0Cyclocarin A is a triterpenoid compound that can be isolated from the leaves of Cyclocarya paliurus. Cyclocarin A shows only weak inhibitory activity against α-glucosidase, lipase, DPP-IV, aldose reductase, and human cancer cell lines (IC50>10 μM).
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Vildagliptin
0 ImagesSynonyms: LAF237; NVP-LAF 237Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.
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Alogliptin
0 ImagesSynonyms: SYR-322 free base
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Teneligliptin
0 ImagesSynonyms: MP-513Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
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Teneligliptin hydrobromide
0 ImagesSynonyms: MP-513 hydrobromideTeneligliptin (MP-513) hydrobromide is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
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Omarigliptin
0 ImagesSynonyms: MK-3102Omarigliptin (MK-3102) is a potent, selective, orally active and cross the blood-brain barrier dipeptidyl peptidase 4 (DPP-4) inhibitor. Omarigliptin shows anti-parkinsonian activity. Omarigliptin has the neuroprotective effect to improve diabetes-associated cognitive dysfunction.
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Sitagliptin phosphate monohydrate
0 ImagesSynonyms: MK-0431 phosphate monohydrateSitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.
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Nateglinide
0 ImagesSynonyms: A4166; SenaglinideNateglinide, 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.
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Anagliptin
0 ImagesSynonyms: SK-0403Anagliptin (SK-0403) 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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Alogliptin Benzoate
0 ImagesSynonyms: SYR 322
