DPP-4/GPR119 modulator 2 is an inhibitor of dipeptidyl peptidase IV (DPP-IV) (IC50: 0.22 μM) and an agonist of GPR119 (EC50: 0.95 μM).

Compound 5a, also known as DPP-4 inhibitor 3, is a powerful dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating an IC50 value of 0.75 nM. It exhibits outstanding antioxidant and insulinotropic activity [1].

DPP-4/GPR119 modulator 1 (Compound 22) is an orally active compound that functions as both a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. It demonstrates a glucose-lowering effect in blood and exhibits moderate inhibition of the hERG channel, with an IC50 value of 4.9 µM. This compound is applicable in diabetes research [1].

DPP-4-IN-8 (compound 27) is a potent and selective inhibitor of dipeptidyl peptidase 4 (DPP4), with an inhibition constant (Ki) of 0.96 μM. It inhibits the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells and dose-dependently reduces the expression of chemokines such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) [1].

DPP-4-IN-2 (compound b2) is a structural analog of Alogliptin that can be used for the research of diabetes. DPP-4-IN-2 is a potent dipeptidyl peptidase 4 (DPP-4) inhibitor with an IC50 value of 79 nM [1].

DPP-4-IN-1 (compound d1) is a highly potent inhibitor of DPP-4 (dipeptidyl peptidase 4) with an IC 50 of 49 nM, making it suitable for diabetes research [1]. It shares structural similarities to Alogliptin and can be effectively utilized for studying diabetes-related mechanisms.

DPP-4-PIOL is an antagonist of GABAA. In dentate gyrus granule cells, it acts by selectively antagonizing tonic over phasic GABAergic currents.

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.

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.

TS-021 is a selective dipeptidyl peptidase 4 (DPP-4) inhibitor with antidiabetic activity for the study of type 2 diabetes.

Cameglipti, a dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type 2 diabetes.

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630/624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

(-)-Sitagliptin carbamoyl glucuronide is a minor phase II metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor (-)-sitagliptin . (-)-Sitagliptin carbamoyl glucuronide is formed by N-carbamoyl glucuronidation and has been found in rat and dog plasma following administration of (-)-sitagliptin.

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

DPP-IV-IN-5, derived from Lycium barbarum fruits, demonstrates moderate agonistic activity towards peroxisome proliferator-activated receptor (PPARγ), showing EC50 values between 10.09 and 44.26 μM, and exhibits inhibitory activity against dipeptidyl peptidase-4 (DPPIV) with an IC50 of 47.13 μM [1].

Vildagliptin carboxylic acid metabolite is the major metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor vildagliptin in humans. Vildagliptin carboxylic acid metabolite has an IC50 value of 477 μM for DPP-4 in human Caco-2 cells. It is formed from hydrolysis of the cyano group on vildagliptin.

Compound 56 (Antidiabetic agent 2) is a glucose-uptake promoter that inhibits DPP-4, PTP-1B, α-amylase, and α-glucosidase, with IC50 values of 0.036, 0.042, 0.241, and 0.185 μM, respectively. This agent effectively decreases blood glucose levels [1].

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

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

BMS-767778, a DPP-4 inhibitor, is used potentially for the treatment of type 2 diabetes.

Imigliptin Dihydrochloride, a selective dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type II diabetes.

Trelagliptin (SYR-472) is a highly specific and long-acting DPP-4 inhibitor.

Anagliptin (SK-0403) is a potent Inhibitor of DPP-4(IC50 of 3.8 nM), for the treatment of type 2 diabetes mellitus.

Denagliptin is a small molecule dipeptidyl peptidase IV (DPP-4) inhibitor for the treatment of endocrine Ü metabolic diseases and can be used in the study of type 2 diabetes.

Saxagliptin is a new oral hypoglycemic of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones and reducing fasting and postprandial glucose conce

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.

Vildagliptin-d7 is a deuterated compound of Vildagliptin. Vildagliptin has a CAS number of 274901-16-5. Vildagliptin 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.

Fluostatin A, a fluorenone compound initially isolated from Streptomyces, demonstrates selective inhibition towards dipeptidyl peptidase 3 (DPP-3) compared to DPP-1, DPP-2, and DPP-4 with IC50 values of 0.44 µg/ml for DPP-3 and over 100 µg/ml for the others, respectively.

Albiglutide fragment (GLP-1 (7-36) analog) TFA represents a biologically active segment of Albiglutide, resistant to DPP-4 degradation due to its structure as a GLP-1 analog. It functions as a long-acting agonist of the GLP-1 receptor, derived from a fusion of a GLP-1 dimer with the human albumin gene. Clinically, this compound demonstrates a pronounced reduction in glycosylated hemoglobin (A1C) levels, rendering it a valuable therapeutic in type 2 diabetes (T2D) research [1] [2] [3] [4].

Besigliptin Tosylate, a DPP-4 inhibitor, is used potentially for the treatment of type 2 diabetes.

Albiglutide TFA, a glucagon-like peptide (GLP)-1 mimetic, is a long acting GLP-1 receptor agonist. Albiglutide TFA significantly reduces glycosylated hemoglobin (A1C). Albiglutide TFA can be used for type 2 diabetes (T2D) research. Albiglutide TFA is generated by the genetic fusion of a DPP-4-resistant GLP-1 dimer to human albumin [1] [2] [3] .

GLP-1(9-36)amide TFA, a predominant metabolite of glucagon-like peptide-1-(7-36)amide synthesized through dipeptidyl peptidase-4 (DPP-4) activity, functions as an antagonist to the human pancreatic GLP-1 receptor [1] [2].

Begelomab (SAND-26), a murine IgG2b monoclonal antibody targeting DPP-4/CD26, has demonstrated utility in investigating severe refractory idiopathic inflammatory myopathy [1] [2].

ASP-4000 free base is a dipeptidyl peptidase 4 (DPP) inhibitor with antihyperglycemic activity.

Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation. Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity.

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

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

Linagliptin-d4 is a deuterated compound of Linagliptin. Linagliptin has a CAS number of 668270-12-0. Linagliptin is a potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity.

Sitagliptin phenylalanine hydrochloride, a dipeptidyl peptidase-4 (DPP-4) inhibitor [1], is a chemical compound utilized in medical applications.

ASP-4000 HCl is an inhibitor of dipeptidyl peptidase 4 (DPP) with anti-hyperglycemic 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.

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.

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.

Sitagliptin fenilalanil is a dipeptidyl aminopeptidase (DPP-4) inhibitor.

Retagliptin is a DPP-4 inhibitor potentially used to treat Type 2 diabetes.

Teneligliptin hydrobromide hydrate is a potent, competitive, and long-lasting DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC 50 s of approximately 1 nM [1].

Linagliptin-13C-d3 the 13C and deuterated compound of Linagliptin. Linagliptin has a CAS number of 668270-12-0. Linagliptin is a potent, orally bioavailable dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity.

Sitagliptin N-sulfate is a phase II metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor (-)-sitagliptin . Sitagliptin N-sulfate is formed via sulfation and has been found in rat bile following oral administration of (-)-sitagliptin.

Fotagliptin benzoate, a Dipeptidyl Peptidase IV (DPP-4) inhibitor with an inhibitory concentration (IC50) of 2.27 nM, demonstrates significant safety in both rat and dog models. It is utilized in Type 2 diabetes mellitus research [1].