dpp-2

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).

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-IV-IN-2 (H-Lys(4-nitro-Z)-pyrrolidide) is an inhibitor of both DP8/9 and dipeptidyl peptidase IV (IC50s: 0.1 and 0.95 μM).

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.

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

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).

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.

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

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].

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

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

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.

ASP8497 is a potent, long-acting DPP-IV inhibitor that improves glucose tolerance by elevating GLP-1 levels in a glucose-dependent insulin-stimulating manner. The compound is used as a therapeutic agent for impaired glucose tolerance and type 2 diabetes.

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.

Nateglinide (Senaglinide) is an oral hypoglycemic agent and amino acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Nateglinide has been linked to rare instances of clinically apparent acute liver injury.

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

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

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.

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

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].

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.

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

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

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts.

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].

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].

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

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.

Vildagliptin dihydrate (LAF237 dihydrate) is a powerful and stable dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating selectivity with an IC50 of 3.5 nM in human Caco-2 cells. This compound exhibits exceptional oral bioavailability and significant antihyperglycemic activity [1].

Alogliptin (SYR-322)(SYR-322) is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10, 000-fold selectivity over DPP-8 and DPP-9.

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].

Teneligliptin (MP-513) is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM. Teneligliptin (MP-513) inhibits all these DPP-4 enzymes in a concentration-dependent manner. The IC50s of Teneligliptin (MP-513) for rhDPP-4, human plasma, and rat plasma are 0.889, 1.75, and 1.35 nM, respectively. A study of enzyme inhibition kinetics is conducted for Teneligliptin (MP-513) using Gly-Pro-MCA as the substrate and rhDPP-4 as the enzyme source. Plots based on the Michaelis-Menten equation reveals that Teneligliptin (MP-513) inhibits DPP-4 in a substrate-competitivemanner; the residual sum of squares for competitive and non-competitive models is 0.162 and 0.192, respectively. Ki, Km, and Vmax values are 0.406 nM, 24 μM, and 6.06 nmol/min, respectively. Teneligliptin (MP-513) inhibits the degradation of GLP-1(7-36)amide with an IC50 of 2.92 nM[1]. Oral administration of Teneligliptin (MP-513) in Wistar rats results in the inhibition of plasma DPP-4 with an ED50 of 0.41 mg/kg. Plasma DPP-4 inhibition is sustained even at 24 h after administration of Teneligliptin (MP-513). An oral carbohydrate-loading test in Zucker fatty rats shows that Teneligliptin (MP-513) at ≥0.1 mg/kg increases the maximum increase in plasmaglucagon-like peptide-1 and insulin levels, and reduces glucose excursions. This effect is observed over 12 h after a dose of 1 mg/kg. An oral fat-loading test in Zucker fatty rats also shows that Teneligliptin (MP-513) at 1 mg/kg reduces triglyceride and free fatty acid excursions. In Zucker fatty rats, repeated administration of Teneligliptin (MP-513) for two weeks reduces glucose excursions in the oral carbohydrate-loading test and decreased the plasma levels of triglycerides and free fatty acids under non-fasting conditions. Oral administration of Teneligliptin (MP-513) inhibits plasma DPP-4 in rats in a dose-dependent manner. The ED50 value for Teneligliptin (MP-513) is calculated to be 0.41 mg/kg, while those for Sitagliptin and Vildagliptin, 27.3 and 12.8 mg/kg, respectively[1]. Teneligliptin (MP-513) improves the histopathological appearance of the liver and decreases intrahepatic triglyceride levels in an NAFLD model mouse, which is associated with downregulation of hepatic lipogenesis-related genes due to AMPK activation[2]. [1]. Fukuda-Tsuru S, et al. A novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor, teneligliptin, improves postprandial hyperglycemia and dyslipidemia after single and repeated administrations. Eur J Pharmacol. 2012 Dec 5;696(1-3):194-202. [2]. Ideta T, et al. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice. Int J Mol Sci. 2015 Dec 8;16(12):29207-18.

Cofrogliptin (HSK7653) (compound 2) is a tetrahydropyran derivative that is an orally active DPP-4 inhibitor with long-lasting hypoglycaemic effects.Cofrogliptin (compound 2) has potential for studies in type 2 diabetes mellitus (T2DM).

Carmegliptin dihydrochloride is the salt form of Camegliptin (free base), also known as RG-1579 and RO4876904, a dipeptidyl peptidase IV (DPP-4) inhibitor potentially for the treatment of type 2 diabetes.

AMG-222 (ALS-2-0426, ALS-20426) is a DPP-4 inhibitor and may be used in the treatment of type 2 diabetes.

Trelagliptin-13C-d3 is the 13C and deuterated compound of Trelagliptin. Trelagliptin has a CAS number of 865759-25-7. Trelagliptin is a highly specific and long-acting DPP-4 inhibitor.