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
-
DPP-4 Related Products (110)
Related Products (110)
-
Anthraquinone-2-carboxylic acid
0 ImagesAnthraquinone-2-carboxylic acid is an orally active anthraquinone compound and Antibacterial agent. Anthraquinone-2-carboxylic acid can be isolated from Bajitian. Anthraquinone-2-carboxylic acid inhibits the activation of DPP-IV, COX-2, NF-κB and AP-1. Anthraquinone-2-carboxylic acid blocks IAV-induced activation of the RIG-I/STAT1 pathway, alleviates IAV-mediated weight loss, and protects against lethal IAV infection. Anthraquinone-2-carboxylic acid inhibits the growth of various Staphylococcus strains. It possesses potent anti-inflammatory, immunomodulatory, analgesic and antibacterial activities.\n
-
Retagliptin phosphate
0 ImagesSynonyms: SP2086 phosphateRetagliptin phosphate (SP2086 phosphate) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin phosphate can be used for type 2 diabetes mellitus (T2DM) research.
-
K579
0 ImagesK579 is a potent and orally active dipeptidyl peptidase IV inhibitor. K579 inhibits the blood glucose elevation. K579 increases the plasma insulin and active forms of glucagon-like peptide-1 (GLP-1). K579 has the potential for the research of diabetic.
-
Saxagliptin hydrochloride
0 ImagesSynonyms: BMS-477118 hydrochlorideSaxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research.
-
Met-Gly-Pro-AMC
0 ImagesMet-Gly-Pro-AMC is a fluorescent peptide substrate active against *Caenorhabditis elegans* DPF-3, hDPP4, and methionyl aminopeptidase 2 (MetAP2). Met-Gly-Pro-AMC undergoes cleavage via tripeptidyl peptidase activity to release a fluorescent product. Met-Gly-Pro-AMC is used to detect the activities of tripeptidyl peptidases and MetAP2 peptidases in in vitro enzyme activity assays.
-
Timosaponin A1
0 ImagesTimosaponin A1, a natural steroidal saponin, is a 5-lipoxygenase (5-LO), COX-2, and dipeptidyl peptidase 4 (DPP-4) inhibitor with IC50s of 3.29 µM, 36.43 µM, and 33.25 µM, respectively.
-
Cofrogliptin
0 ImagesSynonyms: HSK7653Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) .
-
YS110
0 ImagesYS110 is a humanized anti-CD26 (DPP4) IgG1 monoclonal antibody. YS110 induces CD26 nuclear translocation through the caveolin pathway. YS110 inhibits the proliferation of tumor cell by delaying G2/M cell cycle transition. YS110 inhibits the infection of Middle East respiratory syndrome coronavirus (MERS CoV) by blocking the binding of MERS CoV S1 to CD26. YS110 can be used for researches on cancer or infection such as Malignant Mesothelioma and MERS.
-
Linagliptin-d4
0 ImagesSynonyms: BI 1356-d4Linagliptin-d4 is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
-
Gosogliptin
0 ImagesSynonyms: PF-00734200; PF-734200Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
-
Sennidin B
0 ImagesSennidin B is an anthraquinone compound isolated from Cassia angustifolia. Sennidin B is a DPP-4 inhibitor with an IC50 of 39.39 μM. Sennidin B is an insect chitinase inhibitor with a Ki of 80 nM against OfChi-h. Sennidin B competitively inhibits chitinase activity by forming π-π stacking interactions with key tryptophan residues in the active site through a folded conformation. Sennidin B activates PI3K/Akt to promote glucose uptake in adipocytes. Sennidin B can be used for the development of biopesticides and research on type 2 diabetes and metabolism-related signaling pathways.
-
Sitagliptin-d4 phosphate
0 ImagesSynonyms: MK-0431-d4 phosphateSitagliptin-d4 phosphate (MK-0431-d4) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin 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.
-
Saxagliptin hydrate
0 ImagesSynonyms: BMS-477118 hydrateSaxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research.
-
Cichoriin
0 ImagesCichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC50 values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y14R (IC50 = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2.
-
Diprotin A TFA
0 ImagesSynonyms: Ile-Pro-Ile TFADiprotin A TFA (Ile-Pro-Ile TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
-
Azaleatin
0 ImagesAzaleatin is an orally active inhibitor of hQC, NS2B-NS3 protease and E. coli β-glucuronidase, with IC50 values of 1.1 μM, 38.00 μg/mL and 0.57 μM, respectively. Azaleatin inhibits the activities of NF-κB, MyD88, JAK1, TLR4, STAT3, IL-1β, IL-6, COX-2, TNF-α and β-glucuronidase, blocks pro-inflammatory signaling pathways, reduces the levels of ROS, MDA and uric acid, elevates the levels of GPx, GSR, GST, SOD, CAT, HO-1 and GSH, scavenges free radicals and exerts reducing capacity. Azaleatin inhibits the expression of pro-apoptotic proteins Bax, Caspase-9 and Caspase-3, and upregulates the expression of anti-apoptotic protein Bcl-2. Azaleatin reduces the levels of cardiac injury markers, restores cardiac histological structure, inhibits Aβ aggregation, dengue protease activity, hepatic stellate cell proliferation and cancer cell growth, and also exhibits antibacterial activity. Azaleatin can be used in studies related to subchronic cardiotoxicity, Alzheimer's disease, dengue fever, hyperuricemia, liver fibrosis, gastric cancer and bacterial infections.
-
NZ-97
0 ImagesCat. No.: HY-158315Purity: 99.43%NZ-97 is a locally deliverable, lung-retaining dipeptidyl peptidase 4 (DPP4) inhibitor with an IC50 of 18 nM. It exhibits selectivity for DPP8 and DPP9 (with IC50 values of 1.3 μM and 0.6 μM, respectively). NZ-97 inhibits the DPP4 pool in lung-resident cells and epithelial lining fluid, elevates IL-6 and IGF-1 levels, and induces the expansion of type 2 alveolar epithelial cells (AEC2). NZ-97 reduces protein content in bronchoalveolar lavage fluid (BALF), ameliorates lung injury and alleviates pulmonary fibrosis. NZ-97 shows tolerability in untreated Mus musculus mice after intratracheal administration, and does not alter the proliferation or differentiation of lung fibroblasts. NZ-97 can be used in studies related to idiopathic pulmonary fibrosis, acute lung injury and emphysema.
-
Glimepiride sulfonamide
0 ImagesGlimepiride sulfonamide acts as both a DPP-IV inhibitor and an α-Amylase inhibitor. It serves as an intermediate for the synthesis of Glimepiride (HY-B0104). Glimepiride sulfonamide stimulates the production and secretion of insulin. It possesses anti-diabetic potential and can be used in diabetes-related research.
-
Fotagliptin benzoate
0 ImagesSynonyms: SAL067Fotagliptin benzoate is a Dipeptidyl Peptidase IV (DPP-4) inhibitor (IC50=2.27 nM). Fotagliptin benzoate displays great security in rat and dog. Fotagliptin benzoate can be used for Type 2 diabetes mellitus research.
-
Sitagliptin fenilalanil
0 ImagesSitagliptin fenilalanil is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor.
