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Dipeptidyl peptidase 4 (DPP-4) inhibitors block a serine protease that trims dipeptides from incretin hormones. DPP-4, also known as cluster of differentiation 26 (CD26), prefers substrates with proline or alanine at the second position. In 1993 it was shown to cleave glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) and to account for their degradation in human serum. Inhibiting the enzyme therefore prolongs incretin signaling in studies of glucose homeostasis and insulin secretion. Sitagliptin, alogliptin benzoate and linagliptin bind to the active site without forming a covalent bond. Vildagliptin and saxagliptin are cyanopyrrolidines that form a reversible covalent adduct with the catalytic serine. Trelagliptin and gemigliptin add further gliptin scaffolds for structure-activity comparisons.
ZINC000003015356 is a DPP4 inhibitor that selectively blocks the activity of the dipeptidyl peptidase-4 enzyme. This inhibition enhances the availability of incretin hormones, which are crucial for glucose metabolism. ZINC000003015356 is primarily used in research related to diabetes and metabolic disorders, contributing to studies focused on glycemic control and potential therapeutic strategies.
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H-Pro-Pro-Gln-OH is an oligopeptide that acts as a potent inhibitor of dipeptidyl peptidase-IV (DPP-IV). This compound exhibits significant biological activity in modulating insulin secretion and glucose metabolism, making it a valuable tool for diabetes research. Its effective inhibition of DPP-IV may contribute to therapeutic strategies in managing type 2 diabetes and related metabolic disorders.
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DPP-8/9 probe-1 is a selective inhibitor targeting Dipeptidyl Peptidase DPP8/9, designed for use in fluorescence microscopy. This fluorescent probe features a nitrobenzoxadiazole (NBD) tag, demonstrating high affinity for DPP8/9 with an IC50 of 15 nM, while showing minimal activity against related S9 family members (IC50 of 210 nM). DPP-8/9 probe-1 enables visualization of active DPP8/9 in vitro, making it a valuable tool for studying the biological functions and pathways associated with this enzyme in research settings.
Florensocatib hydrate is a potent inhibitor of dipeptidyl peptidase I (DPP1) with an IC50 value of 1.6 nM. This compound exhibits favorable bioavailability and pharmacokinetic properties, making it suitable for studies investigating inflammatory diseases and related pathophysiological processes. Its ability to modulate DPP1 activity provides a valuable tool for understanding disease mechanisms and exploring potential therapeutic strategies.
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AMG-222 is a dipeptidyl peptidase IV (DPP-IV) inhibitor that reversibly binds to the enzyme, thereby inhibiting its activity. This compound demonstrates a saturable and concentration-dependent binding to human plasma proteins, achieving a binding rate of 80.8% at 1 nM and decreasing to 29.4% at concentrations above 100 nM. AMG-222 is primarily utilized in diabetes research, aiding studies focused on glucose metabolism and insulin regulation.
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BMS-767778 is a selective DPP4 inhibitor, exhibiting high affinity with Ki values of 0.94 nM for DPP4, and 4.9 nM and 3.2 nM for DPP8 and DPP9, respectively, demonstrating over 3,000-fold selectivity against these related enzymes. This compound also inhibits CYP-3A4 with an IC50 of 5.2 μM. BMS-767778 has been shown to significantly lower blood glucose levels in high-fat diet-induced ob/ob mouse models, indicating its potential for diabetes mellitus research applications.
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DPP-4-IN-1 is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4) with an IC50 of 49 nM. This compound, structurally analogous to Alogliptin, plays a crucial role in regulating glucose metabolism and enhancing insulin secretion. DPP-4-IN-1 is essential for diabetes research, facilitating investigations into therapeutic strategies for managing hyperglycemia.
Denagliptin tosylate is a tosyate salt of Denagliptin, functioning as a potent dipeptidyl peptidase IV (DPP-4) inhibitor. This small molecule effectively enhances incretin levels, contributing to improved glycemic control in type 2 diabetes models. Its applications in research include investigating mechanisms of insulin secretion and glucose metabolism, making it a valuable tool for diabetes-related studies.
DPP-4-IN-9 is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4) with an IC50 of 8.22 nM. This compound exhibits significant antihyperglycemic activity, making it a valuable tool for research in diabetes and metabolic disorders. DPP-4-IN-9 is suitable for studies aimed at understanding the role of DPP-4 in glucose metabolism and the development of therapeutic agents targeting this pathway.
Gosogliptin hydrochloride is a selective, competitive inhibitor of DPP-IV, an enzyme crucial for the degradation of incretin peptides such as GLP-1 and glucose-dependent insulinotropic polypeptide. This compound exhibits rapid and reversible inhibition of plasma DPP-4 activity, leading to enhanced insulin secretion and improved glucose tolerance. Gosogliptin hydrochloride is primarily utilized in research focused on diabetes and metabolic disorders, providing valuable insights into glucose regulation and insulin dynamics.
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BMS-538305 hydrochloride is a potent and selective inhibitor of dipeptidyl peptidase IV (DPP-IV), exerting its biological activity through the formation of a reversible covalent complex with the enzyme. The mechanism of action involves the covalent binding between the nitrile carbon of BMS-538305 and the enzyme residue S630, as revealed by X-ray crystal structure analysis. This compound is primarily utilized in research related to glucose metabolism and diabetes management, making it valuable for studies focused on metabolic disorders and therapeutic development.
Florensocatib is a potent inhibitor of Dipeptidyl Peptidase I (DPP1), a key enzyme involved in the processing of pro-inflammatory cytokines. This compound exhibits significant biological activity, making it a valuable tool for research in bronchiectasis and related inflammatory diseases. Its selective inhibition of DPP1 provides insights into therapeutic strategies aimed at modulating immune responses.
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DPP-4-IN-2 is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4) with an IC50 of 79 nM. This compound serves as a structural analog of Alogliptin and is primarily utilized in diabetes research. DPP-4-IN-2 facilitates the investigation of glucose metabolism and insulin signaling pathways, making it a valuable tool for understanding the pathophysiology of type 2 diabetes and developing potential therapeutic strategies.
Synonyms: RO-4876904
Carmegliptin is a potent and orally active DPP-IV inhibitor, demonstrating an IC50 value of 6.8 nM for human DPP-IV. By binding to the S1 pocket of DPP-IV, it effectively inhibits the degradation of GLP-1, leading to increased plasma insulin levels, improved glucose tolerance, and alleviation of hyperglycemia. Carmegliptin serves as a substrate for human P-glycoprotein without inhibiting the transporter, exhibiting low in vitro cell permeability. This compound is valuable for research focused on type 2 diabetes and non-insulin-dependent diabetes mellitus.
DPP-1-IN-1 is a potent inhibitor of Cathepsin C (Dipeptidyl peptidase I) with an IC50 of 5.31 nM. It effectively inhibits the activity of Cathepsin C, subsequently affecting Neutrophil elastase in neutrophils. This compound is valuable for research in the field of inflammatory diseases, providing insights into mechanisms of inflammation and potential therapeutic pathways.
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TAK-100 is a selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitor, exhibiting an IC50 of 5.3 nM. This compound demonstrates minimal inhibitory effects on other dipeptidyl peptidases, highlighting its specificity. TAK-100 is primarily utilized in research focused on diabetes, facilitating the exploration of glucose metabolism and insulin regulation.
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Propyl-GSK-2793660 is an irreversible and covalent inhibitor of Dipeptidyl Peptidase I (DPP1). This compound exhibits significant biological activity in the modulation of DPP1 activity, making it a valuable tool for studying conditions related to bronchiectasis. Its specificity and mechanism of action can facilitate research on the implications of DPP1 inhibition in various biological contexts.
Synonyms: LC15-0444 hydrochloride
Gemigliptin hydrochloride is a selective and reversible inhibitor of dipeptidyl peptidase-4 (DPP-4), with an IC50 of 10.3 nM for human recombinant DPP-4. This compound demonstrates significant anti-glycation properties, making it a valuable tool in the study of advanced glycation end products (AGE) and their association with diabetic complications. Gemigliptin hydrochloride is primarily utilized in research focused on the modulation of glucose metabolism and the management of diabetes-related conditions.
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Melogliptin is a DPP-4 inhibitor that plays a crucial role in modulating glucose metabolism. By inhibiting the DPP-4 enzyme, Melogliptin enhances incretin levels, leading to improved insulin secretion and reduced glucagon levels. This compound is primarily utilized in research targeting type 2 diabetes and related metabolic disorders, providing insights into potential therapeutic strategies for glucose regulation.
MK-0626 is a selective Dipeptidyl Peptidase-4 (DPP-4) inhibitor, exhibiting an IC50 of 6.3 nM. This compound enhances endothelial nitric oxide synthase expression and is effective in promoting neovascularization. MK-0626 demonstrates potential in mitigating hepatic steatosis and pancreatic islet injury. It is particularly relevant in research focused on diabetes and non-alcoholic fatty liver disease.
Synonyms: RO-4876904 (hydrochloride)
Carmegliptin hydrochloride is a potent DPP-IV inhibitor, exhibiting a human DPP-IV IC50 of 6.8 nM. By binding to the S1 pocket of DPP-IV, it prevents the degradation of GLP-1, leading to increased plasma insulin levels, improved glucose tolerance, and relief from hyperglycemia. This compound can serve as a valuable reagent for research into type 2 diabetes and non-insulin-dependent diabetes mellitus, providing insights into GLP-1 modulation and its effects on metabolic regulation.
Sulphostin is a covalent inhibitor targeting dipeptidyl peptidase 4 (DPP4), dipeptidyl peptidase 9 (DPP9), and dipeptidyl peptidase 8 (DPP8) with IC50 values of 79, 1392, and 6930 nM, respectively. By inducing phosphosulfamate modification, Sulphostin irreversibly inhibits these enzyme activities, making it a valuable tool in the study of inflammatory processes and cancer research. Its selective inhibition profile allows for detailed investigation into the roles of DPPs in various biological pathways.
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P32/98 hemifumarate is a potent dipeptidyl peptidase IV (DPP4) inhibitor with a Ki value of 130 nM. It has been shown to enhance glucose tolerance, improve insulin sensitivity, and increase β-cell responsiveness in a fatty Zucker rat model. This compound is valuable for research applications focused on diabetes and metabolic disorders, providing insights into DPP4 inhibition mechanisms and their effects on glucose homeostasis.
DPP9-IN-1 is a selective inhibitor of dipeptidyl peptidase 9 (DPP9) with an IC50 value of 3 nM, also exhibiting inhibition of DPP8 at 0.6 μM. This compound has been shown to induce concentration-dependent lactate dehydrogenase (LDH) release in THP-1 cells, indicating potential cytotoxic effects. DPP9-IN-1 is useful in research applications related to immune response modulation and study of DPP9-related pathways in cellular processes.
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P32/98 is a potent dipeptidyl peptidase IV (DPP4) inhibitor, exhibiting a Ki value of 130 nM. This compound is notable for its ability to enhance glucose tolerance, improve insulin sensitivity, and increase β-cell responsiveness, specifically in the fatty Zucker rat model. P32/98 is suitable for research applications targeting metabolic disorders and studying glucose homeostasis.
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