dpp

DPP-IV-IN-1 is an effective inhibitor of dipeptidyl peptidase IV (DPP-IV), a serine protease (IC50: 4.6 nM).

5,15-Diphenylporphyrin (5,15-DPP) is a selective STAT3-SH2 antagonist with IC50 values of 0.28 μM for STAT3 and 10 μM for STAT1 [1].

NVP-DPP728 is a potent, reversible, nitrile-dependent inhibitor of dipeptidyl peptidase IV (DPP-IV) with an inhibition constant (K i) of 11 nM for human DPP-IV amidolytic activity. By inhibiting the degradation of glucagon-like peptide-1 (GLP-1), NVP-DPP728 enhances insulin release following glucose intake, making it useful for diabetes research [1].

NVP-DPP728 dihydrochloride is a highly potent, selective, and orally active inhibitor of dipeptidyl peptidase IV (DPP-IV), with a binding affinity (K i ) of 11 nM. This compound proves useful for investigating diabetes mellitus in research studies.

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

Linagliptin (BI 1356) is a potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity.

Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein/enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.

Vildagliptin (LAF237) is a cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Vildagliptin's cyano moiety undergoes hydrolysis and this inactive metabolite is excreted mainly via the urine.

Trelagliptin succinate (SYR-472 succinate) is a long-acting inhibitor of dipeptidyl peptidase-4 (DPP-4), being developed for the treatment of type 2 diabetes (T2D).

Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.

Alogliptin Benzoate (SYR 322)(SYR 322), an effective and specific DPP-4 inhibitor (IC50<10 nM), exhibits greater than 10, 000-fold selectivity over DPP-8/9. Alogliptin may inhibit inflammatory responses by preventing the toll-like receptor 4 (TLR-4)-mediated formation of proinflammatory cytokines.

Teneligliptin hydrobromide (MP-513 (hydrobromide)) is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus.

DBPR108 is an orally bioavailable dipeptide-derived DPP4 inhibitor (IC50: 15 nM) and it has no inhibition on DDP8 and DPP9.

Retagliptin Phosphate (SP 2086) is pharmaceutical composition of DPP-4 inhibitor, for treating type-2 diabetes.

Saikogenin A is a dipeptidyl peptidase-4 inhibitor.

Talabostat mesylate (PT100) is an orally active, selective inhibitor of dipeptidyl peptidases IV (DPP4, IC50: 0.18 nM), including tumor-associated fibroblast activation protein. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony-stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis.

UAMC00039 dihydrochloride is a potent, reversible, and competitive inhibitor of dipeptidyl peptidase II, with an IC50 of 0.48 nM.

Saxagliptin (BMS-477118) is a selective, reversible DPP4 inhibitor with an IC50 of 26 nM.

Gemigliptin (LC15-0444) is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor(KD : 7.25 nM.)

Gemigliptin Tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive inhibitor of dipeptidyl peptidase-4 (DPP-4). It has an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties.

NDMC101 is an inhibitor of dipeptidyl peptidase-IV activity in human T cells and exhibits immunomodulatory effects. It also acts as a novel inhibitor of NFATc1 and NF-κB activity.

Azaleatin is a natural product from Rhododendron simsii. Azaleatin is a dipeptidyl peptidase-IV inhibitor. Azaleatin can be used for type-2 diabetes and obesity studies.

Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively).