2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Dipeptidyl Peptidase
  5. DPP-4 Isoform

DPP-4

DPP-4 (DPP IV) belongs to the family of serine proteases, comprising of 766 amino acids. It is composed of a 6-amino-acid cytoplasmic tail, a transmembrane domain of 22-amino-acids, and a large extracellular domain. The extracellular domain is responsible for ligand binding and for DPP-4 activity. DPP-4 is a soluble plasma enzyme expressed in high levels in the capillary bed of the gut mucosa, some immune cells like T cells and epithelial cells. DPP-4 is also expressed in other organs such as the liver, the intestine, the kidney and the lungs. The imprecise expression of soluble DPP-4 leads to many biological disorders including solid tumors, diabetes mellitus (type-2), obesity, autoimmune diseases and hepatitis.Dipeptidyl peptidase IV is well known for its role in glucose homeostasis. It has become a validated therapeutic target for the treatment of type 2 diabetes (T2D).

DPP-4 Related Products (100):

Cat. No. Product Name Effect Purity
  • HY-13749
    Sitagliptin
    		Inhibitor 99.94%
    Sitagliptin (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.
  • HY-13233A
    Talabostat mesylate
    		Inhibitor 98.35%
    Talabostat 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.
  • HY-10284
    Linagliptin
    		Inhibitor 99.74%
    Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
  • HY-111174
    Diprotin A
    		Inhibitor 99.90%
    Diprotin A (Ile-Pro-Ile) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
  • HY-13749A
    Sitagliptin phosphate
    		Inhibitor 99.88%
    Sitagliptin (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.
  • HY-Z1764
    DPP-4-IN-18
    		Inhibitor
    DPP-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.
  • HY-153522
    ZY15557
    		Inhibitor
    ZY15557 is a novel, competitive, long acting, orally active DPP-4 inhibitor, with a Ki of 5.53 nM. ZY15557 inhibits plasma DPP-4 activity. ZY15557 can be used in the research of type 2 diabetes.
  • HY-182580
    HBK001
    		Inhibitor
    HBK001 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.
  • HY-14291
    Vildagliptin
    		Inhibitor 99.93%
    Vildagliptin (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.
  • HY-116304
    1G244
    		Inhibitor 98.50%
    1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
  • HY-10285
    Saxagliptin
    		Inhibitor 99.96%
    Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research.
  • HY-A0023A
    Alogliptin
    		Inhibitor 99.93%
    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.
  • HY-14806A
    Teneligliptin hydrobromide
    		Inhibitor 99.99%
    Teneligliptin (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.
  • HY-14806
    Teneligliptin
    		Inhibitor 99.79%
    Teneligliptin (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.
  • HY-15981
    Omarigliptin
    		Inhibitor 99.96%
    Omarigliptin (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.
  • HY-15408
    Trelagliptin
    		Inhibitor 99.81%
    Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).
  • HY-13749B
    Sitagliptin phosphate monohydrate
    		Inhibitor 99.83%
    Sitagliptin (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.
  • HY-B0422
    Nateglinide
    		Inhibitor 99.95%
    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.
  • HY-14877
    Anagliptin
    		Inhibitor 99.92%
    Anagliptin (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.
  • HY-A0023
    Alogliptin Benzoate
    		Inhibitor 99.98%
    Alogliptin Benzoate (SYR-322) 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 Benzoate can be used for the research of type 2 diabetes.