2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Dipeptidyl Peptidase

Dipeptidyl Peptidase

DPP

Dipeptidyl Peptidase

Related Products

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Dipeptidyl Peptidases are widely distributed exopeptidases that possess central role in proteolysis. The dipeptidyl peptidase family, including DPP-IV DPP7, DPP8, DPP9, fibroblast activation protein and others, cleave the peptide bond after the penultimate proline residue and are drug target rich.

DPP-IV (DPP4 or CD26) is a serine protease detected on several immune cells and on epithelial cells of various organs. Besides the membrane-bound enzyme, a catalytically active soluble form is detected in several body fluids. Both variants cleave off dipeptides from the N-termini of various chemokines, neuropeptides, and hormones. DPP IV plays a key role in immune-regulation, inflammation, oxidative stress, cell adhesion, and apoptosis by targeting different substrates. DPP IV inhibitors are commonly used as hypoglycemic agents.

DPP8 and DPP9 show DPPIV-like activity and share a very high-sequence similarity to each other. DPP8 and DPP9 are intracellular N-terminal dipeptidyl peptidases (preferentially postproline) associated with pathophysiological roles in immune response and cancer biology.

Dipeptidyl Peptidase Isoform Specific Products:

Dipeptidyl Peptidase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13749R
    Sitagliptin (Standard)
    		Inhibitor
    Sitagliptin (Standard) is the analytical standard of Sitagliptin (HY-13749). This product is intended for research and analytical applications. Sitagliptin 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.
    Sitagliptin (Standard)
  • HY-15408AR
    Trelagliptin succinate (Standard)
    		Inhibitor
    Trelagliptin (succinate) (Standard) is the analytical standard of Trelagliptin (succinate). This product is intended for research and analytical applications. Trelagliptin (SYR-472) succinate 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).
    Trelagliptin succinate (Standard)
  • HY-13749CR
    (S)-Sitagliptin phosphate (Standard)
    		Inhibitor
    (S)-Sitagliptin (phosphate) (Standard) is the analytical standard of (S)-Sitagliptin (phosphate). This product is intended for research and analytical applications. (S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (S)-Sitagliptin phosphate (Standard)
  • HY-180527
    SGLT2-IN-5
    		Inhibitor
    SGLT2-IN-5 (Compound 99) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 23, and 58 nM respectively. SGLT2-IN-5 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-5 can be used for the study of type 2 diabetes.
    SGLT2-IN-5
  • HY-14806R
    Teneligliptin (Standard)
    		Inhibitor
    Teneligliptin (Standard) is the analytical standard of Teneligliptin. This product is intended for research and analytical applications. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM.
    Teneligliptin (Standard)
  • HY-N8134
    2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one
    		Inhibitor 99.70%
    2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one is a natural product found in the leaves and stem bark of M. glabra. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one displays binding affinities with dipeptidyl peptidase-4 (DPP-4) and α-Amylase. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one has potential antidiabetic activities.
    2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one
  • HY-170800
    DPP-4-IN-15
    		Inhibitor
    DPP-4-IN-15 (Compound 22) is a non-competitive inhibitor of dipeptidyl peptidase-4 (DPP-4) with an IC50 of 8.24 μM.
    DPP-4-IN-15
  • HY-10285AR
    Saxagliptin hydrate (Standard)
    		Inhibitor
    Saxagliptin (hydrate) (Standard) is the analytical standard of Saxagliptin (hydrate). This product is intended for research and analytical applications. Saxagliptin 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.
    Saxagliptin hydrate (Standard)
  • HY-175590
    DPP-4-IN-17
    		Inhibitor
    DPP-4-IN-17 is an orally active and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 value of 0.12 nM. DPP-4-IN-17 increases the enzyme's Km value (75.73 μM vs. 27.18 μM of substrate alone) and reduces catalytic efficiency. DPP-4-IN-17 reduces blood glucose levels and reverses weight loss in Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150)-induced diabetic rats. DPP-4-IN-17 can be used for the study of type 2 diabetes mellitus (T2DM).
    DPP-4-IN-17
  • HY-14291R
    Vildagliptin (Standard)
    		Inhibitor
    Vildagliptin (Standard) is the analytical standard of Vildagliptin. This product is intended for research and analytical applications. 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.
    Vildagliptin (Standard)
  • HY-13749S3
    Sitagliptin-d6
    		Inhibitor
    Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin 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.
    Sitagliptin-d<sub>6</sub>
  • HY-10285S1
    (rel)-Saxagliptin-13C,d2 TFA
    		Inhibitor
    (rel)-Saxagliptin-13C,d2 ((rel)-BMS-477118-13C,d2) TFA is 13C-labeled Saxagliptin (HY-10285).
    (rel)-Saxagliptin-<sup>13</sup>C,d<sub>2</sub> TFA
  • HY-108319R
    DPP-IV-IN-2 (Standard)
    		Inhibitor
    DPP-IV-IN-2 (Standard) is the analytical standard of DPP-IV-IN-2 (HY-108319). This product is intended for research and analytical applications. DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively.
    DPP-IV-IN-2 (Standard)
  • HY-132489S
    (Rac)-Sitagliptin-d4
    		Inhibitor
    (Rac)-Sitagliptin-d4 ((Rac)-MK-0431-d4) is the deuterium labeled (Rac)-Sitagliptin. (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (Rac)-Sitagliptin-d<sub>4</sub>
  • HY-N14989A
    Fluostatin A sodium
    		Inhibitor
    Fluostatin A sodium is a dipeptidyl peptidaseIII inhibitor with an IC50 of 0.44 μg/mL. Fluostatin A can be extracted from Streptomyces sp. TA-3391.
    Fluostatin A sodium
  • HY-N14989
    Fluostatin A
    		Inhibitor
    Fluostatin A inhibits the ability of DPP-III, and with arginyl-arginine-2-naphthalene formamide as the substrate, the IC50 is 0.44 μg/mL.
    Fluostatin A
  • HY-180528
    SGLT2-IN-6
    		Inhibitor
    SGLT2-IN-6 (Compound 101) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 6.7, and 72 nM respectively. SGLT2-IN-6 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-6 can be used for the study of type 2 diabetes.
    SGLT2-IN-6
  • HY-14806S2
    Teneligliptin-d5
    		Inhibitor
    Teneligliptin-d5 (MP-513-d5) is deuterium labeled Teneligliptin. 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.
    Teneligliptin-d<sub>5</sub>
  • HY-151871A
    cis-ICeD-2
    		Inhibitor
    cis-ICeD-2 is the cis isomer of ICeD-2 (HY-151871). ICeD-2 is a cell death inducer that induces cell death in HIV-1-infected cells. ICeD-2-mediated killing of HIV-1-infected cells is dependent on HIV-1 protease activity. ICeD-2 effectively blocks the hydrolysis of Gly-Pro-AMC by the dipeptidyl peptidases DPP8 and DPP9. ICeD-2 demonstrates strong stability against DPP9 in PBMCs..
    cis-ICeD-2
  • HY-132489S1
    (Rac)-Sitagliptin-d4-1 hydrochloride
    		Inhibitor
    (Rac)-Sitagliptin-d4-1 hydrochloride ((Rac)-MK-0431-d4-1 hydrochloride) is the deuterium labeled (Rac)-Sitagliptin-1 hydrochloride. (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (Rac)-Sitagliptin-d<sub>4</sub>-1 hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Dipeptidyl Peptidase Isoform Comparison

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