dpp-iv

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

Dipeptidyl peptidase-IV (DPP-IV) is an enzyme that deactivates incretin hormones such as glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which are crucial in regulating blood glucose levels. Additionally, DPP-IV functions as a binding protein and ligand for various extracellular molecules. This enzyme is instrumental in research related to diabetes and cancer.

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).

DPP IV hCA II-IN-1 is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA), exhibiting an IC50 of 0.049 μM for DPP IV and K_i values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively [1].

Cameglipti, a dipeptidyl peptidase IV (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.

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.

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

MK-0626 is an orally available dipeptidyl peptidase IV (DPP-4) inhibitor that attenuates hepatic steatosis and accumulation by enhancing AMPK activity.MK-0626 attenuates TAC-induced diabetic pancreatic islet injury by restoring the expression of GLP-1R.MK-0626 is able to increase circulating endothelial progenitor cell numbers and endothelial-type nitric oxide synthase expression by promoting neoangiogenesis.

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.

Ficusonolide exhibits significant antidiabetic activity through its interactions with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.

DPPI 1c hydrochloride is an inhibitor of dipeptidyl peptidase IV (IC50 = 104 nM) that shows selectivity over enzymes with DPP-like activity (IC50 > 30 μM).

Gosogliptin is a potent, orally active, highly selective and competitive inhibitor of DPP-4 (dipeptidyl peptidase 4), increasing the levels of intestinal glucagon peptide (GLP-1) and glucose-dependent proinsulinotropic polypeptide (GIP), thereby enhancing insulin secretion and lowering blood glucose levels. In animal studies, Gosogliptin rapidly, orally and reversibly inhibits plasma DPP-4 activity.

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.

Prodipine hydrochloride for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit (IC50 of 4.5 μM and 30 μM, respectively).

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.

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, a Platinum(IV) complex with a pterostilbene-derived axial ligand, inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, demonstrating antiproliferative activity. It activates caspase-3 and cleaved poly ADP-ribose polymerase, inducing apoptosis. Furthermore, DPP enhances the maturation and antigen presentation of dendritic cells and exhibits in vivo safety [1].

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].

AMG-222 tosylate is a DPP-IV inhibitor in clinical development for type II diabetes.

VAMP is a tetrapeptide that acts as a competitive dipeptidyl peptidase IV (DPP-IV) inhibitor, exhibiting an IC50 of 1.00 μM and a Kd of 6.89 μM. It effectively targets the DPP-IV-GLP-1 axis and is utilized in the research of type 2 diabetes.

γ-Glu-Tyr (gamma-Glutamyltyrosine) is a kokumi peptide with competitive inhibition of dipeptidyl peptidase-IV (DPP-IV) and is used in the study of diabetes mellitus.

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.