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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.
Synonyms: MP-513 hydrobromide hydrate; MP513
Teneligliptin hydrobromide hydrate 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.
Synonyms: Ile-Pro-Pro (TFA)
Diprotin A (TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
Synonyms: PF-00734200; PF-734200
Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
Synonyms: PHX-1149 free base; PHX1149
Dutogliptin (PHX-1149 free base) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.
Synonyms: LAF237 dihydrate; NVP-LAF 237 dihydrate; LAF 237
Vildagliptin (LAF237 dihydrate;NVP-LAF 237 dihydrate) is a dipeptidyl peptidase 4 (DPP4) inhibitor that delays the degradation of glucagon-like peptide-1 (GLP-1).
γ-Glu-Tyr, a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV) (IC50=6.77 mM), is a potentially functional component of the type 2 diabetes diet.
DPP4-In hydrochloride is a selective inhibitor of dipeptidyl peptidase 4 (DPP4), an enzyme that plays a critical role in glucose metabolism and immune regulation. By inhibiting DPP4, this compound can effectively increase the levels of active incretin hormones, which may contribute to improved glycemic control. DPP4-In hydrochloride is primarily utilized in diabetes research and can aid in the investigation of metabolic disorders and potential therapeutic strategies for type 2 diabetes.
Synonyms: MK-0431 phosphate
Sitagliptin phosphate is a selective DPP4 inhibitor with a powerful mechanism of action, featuring an IC50 value of 19 nM. By inhibiting DPP4, this compound prevents the degradation of incretins such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), resulting in enhanced active incretin levels. Additionally, it can directly stimulate GLP-1 secretion from intestinal L cells via the cAMP/PKA and ERK1/2 pathways, which operates independently of DPP-4. Sitagliptin phosphate is valuable for researching both type 1 and type 2 diabetes and demonstrates protective effects on pancreatic islet grafts in type 1 diabetes models.
Synonyms: MK-0431 hydrochloride
Sitagliptin hydrochloride is a selective DPP4 inhibitor, demonstrating an IC50 of 19 nM. By inhibiting DPP4, this compound prevents the breakdown of incretin hormones, such as GLP-1 and GIP, ultimately increasing their active levels. Additionally, sitagliptin can stimulate GLP-1 secretion from intestinal L cells via the cAMP/PKA and ERK1/2 pathways, independent of DPP-4 inhibition. This reagent is applicable in research involving type 1 and type 2 diabetes, and it also exhibits protective effects on pancreatic islet grafts in type 1 diabetes models.
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PB01 is a selective DPP-4 inhibitor with an IC50 of 15.66 nM. It effectively reduces high glucose-induced reactive oxygen species (ROS) production and mitochondrial superoxide generation while significantly decreasing cellular DPP-4 expression. In vivo studies demonstrate that PB01 can lower blood glucose levels in diabetic mice, indicating its potential therapeutic application. Furthermore, PB01 exhibits minimal cytotoxicity at a concentration of 100 μM, making it a promising candidate for diabetes-related research.
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DPP-4-IN-3 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), exhibiting an IC50 value of 0.75 nM. This compound demonstrates significant antioxidant properties alongside insulinotropic activity, making it a valuable tool for diabetes research and the study of metabolic disorders. Its ability to modulate the DPP-IV pathway underscores its potential in therapeutic applications aimed at enhancing glucose homeostasis.
Synonyms: DA-1229 tartrate
Evogliptin tartrate is an orally active DPP4 inhibitor that exhibits significant and sustained hypoglycemic effects in murine models. It not only lowers blood glucose levels but also attenuates the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. This compound is suitable for research applications related to type 2 diabetes, osteoporosis, renal impairment, and chronic liver inflammation.
Synonyms: DA-1229
Evogliptin is an orally active inhibitor of DPP4 (dipeptidyl peptidase-4), demonstrating notable and sustained hypoglycemic effects in murine models. In addition to its antidiabetic properties, Evogliptin exerts effects by inhibiting the production of inflammatory and fibrotic signals in hepatocytes through the induction of autophagy. This compound is particularly relevant for research applications related to type 2 diabetes, osteoporosis, renal impairment, and chronic liver inflammation.
Synonyms: (S)-MK-0431 phosphate
(S)-Sitagliptin phosphate functions as a dipeptidyl peptidase 4 (DPP4) inhibitor, exhibiting a potent inhibitory effect with an IC50 of 19 nM in Caco-2 cell extracts. This compound demonstrates significant biological activity in the regulation of glucose metabolism and is primarily used in research focused on diabetes and metabolic disorders. Its potent inhibition of DPP4 makes it a valuable reagent for studies investigating therapeutic strategies to manage hyperglycemia and related conditions.
Synonyms: (Rac)-MK-0431
(Rac)-Sitagliptin is a potent and selective inhibitor of dipeptidyl peptidase-4 (DPP4), exhibiting an IC50 of 19 nM in Caco-2 cell extracts. This compound plays a significant role in the modulation of glucose metabolism, making it relevant for diabetes research. Its ability to enhance insulin secretion and decrease glucagon levels underscores its potential applications in studying metabolic disorders and developing therapeutic strategies for type 2 diabetes.
DPP IV/hCA II-IN-1 is a potent and selective inhibitor of dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA) enzymes. This compound exhibits a strong inhibitory effect on DPP IV with an IC50 value of 0.049 μM, while displaying varying Ki values for different carbonic anhydrase isoforms, including 0.0361 μM for CA II. Its dual-target inhibitory activity makes it a valuable tool for studying metabolic disorders and exploring therapeutic avenues in conditions involving DPP IV and CA dysregulation.
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D-γ-Glu-Tyr is a D-isomer of γ-Glu-Tyr, distinguished by its γ-glutamyl content. This compound acts as a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV), exhibiting an IC50 value of 6.77 mM. D-γ-Glu-Tyr is relevant in the study of type 2 diabetes and may serve as a functional component in dietary approaches to manage this condition.
Val-Pyrrolidide hydrochloride is a potent Dipeptidyl Peptidase IV (DPPIV) inhibitor. This compound effectively prevents the N-terminal truncation of the peptide Gln3-Aβ(1–11), making it a valuable tool for studies investigating the role of DPPIV in neurodegenerative diseases. Val-Pyrrolidide hydrochloride can facilitate research into peptide processing and potential therapeutic interventions in Alzheimer's disease.
Synonyms: Ile-Pro-Ile
Diprotin A, an inhibitor of dipeptidyl peptidase IV (DPP-IV), plays a crucial role in modulating the degradation of incretin hormones. By inhibiting DPP-IV activity, Diprotin A enhances insulin secretion and glucose tolerance, making it relevant in diabetes research and metabolic studies. Its application extends to investigating the mechanisms of peptide regulation and therapeutic interventions in glucose metabolism disorders.
Synonyms: LC15-0444 tartrate
Gemigliptin tartrate is a selective and reversible inhibitor of dipeptidyl peptidase-4 (DPP-4), demonstrating an IC50 of 10.3 nM for human recombinant DPP-4. This compound exhibits significant anti-glycation properties, making it valuable for research into advanced glycation end products (AGEs) and their associated diabetic complications. Its specificity and efficacy position Gemigliptin tartrate as a useful tool in studies aimed at understanding and mitigating the effects of diabetes-related conditions.
Synonyms: BMS-477118 hydrochloride
Saxagliptin hydrochloride is a potent, selective, reversible inhibitor of dipeptidyl peptidase-4 (DPP-4), exhibiting an inhibition constant (Ki) of 0.6-1.3 nM. This compound is primarily employed in research focused on type 2 diabetes mellitus, as it enhances insulin secretion by increasing incretin levels, aiding in glucose regulation. Saxagliptin hydrochloride serves as a valuable tool for studying DPP-4's role in glucose homeostasis and potential therapeutic interventions in diabetes management.
Synonyms: SP2086
Retagliptin is a selective, competitive inhibitor of dipeptidyl peptidase-4 (DPP-4) known for its oral bioavailability. It plays a crucial role in increasing incretin levels, which enhances insulin secretion and lowers glucagon levels in patients with type 2 diabetes mellitus (T2DM). This compound is valuable for research applications focused on the regulation of glucose homeostasis and the therapeutic potential in metabolic disorders.
Synonyms: HSK7653
Cofrogliptin is a potent oral dipeptidyl peptidase-4 (DPP-4) inhibitor. It exhibits long-acting antidiabetic efficacy, making it a promising candidate for the management of type 2 diabetes mellitus (T2DM). Cofrogliptin's mechanism of action enhances incretin levels, which supports insulin secretion and regulates glucose metabolism. This compound is valuable for research applications focused on diabetes treatment and metabolic disorders.
Synonyms: LC15-0444 tartrate hydrate
Gemigliptin tartrate hydrate is a selective and reversible inhibitor of dipeptidyl peptidase-4 (DPP-4), exhibiting an IC50 of 10.3 nM against human recombinant DPP-4. This compound demonstrates significant anti-glycation activity and is a valuable tool for investigating advanced glycation end products (AGEs) in the context of diabetic complications. Its application in research can help elucidate the mechanisms underlying AGE-related pathologies.
