Dipeptidyl Peptidase Inhibitor

Trelagliptin (SYR-472) succinate is a potent, orally active and highly selective DPP-4 inhibitor with an IC₅₀ of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).

Evogliptin (DA-1229) tartrate is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.

Anthraquinone-2-carboxylic acid is an orally active anthraquinone compound and Antibacterial agent. Anthraquinone-2-carboxylic acid can be isolated from Bajitian. Anthraquinone-2-carboxylic acid inhibits the activation of DPP-IV, COX-2, NF-κB and AP-1. Anthraquinone-2-carboxylic acid blocks IAV-induced activation of the RIG-I/STAT1 pathway, alleviates IAV-mediated weight loss, and protects against lethal IAV infection. Anthraquinone-2-carboxylic acid inhibits the growth of various Staphylococcus strains. It possesses potent anti-inflammatory, immunomodulatory, analgesic and antibacterial activities.\n

Retagliptin phosphate (SP2086 phosphate) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin phosphate can be used for type 2 diabetes mellitus (T2DM) research.

Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC₅₀ of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

K579 is a potent and orally active dipeptidyl peptidase IV inhibitor. K579 inhibits the blood glucose elevation. K579 increases the plasma insulin and active forms of glucagon-like peptide-1 (GLP-1). K579 has the potential for the research of diabetic.

Retagliptin (SP2086) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin can be used for type 2 diabetes mellitus (T2DM) research.

Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (K_i = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research.

Timosaponin A1, a natural steroidal saponin, is a 5-lipoxygenase (5-LO), COX-2, and dipeptidyl peptidase 4 (DPP-4) inhibitor with IC₅₀s of 3.29 µM, 36.43 µM, and 33.25 µM, respectively.

Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) .

YS110 is a humanized anti-CD26 (DPP4) IgG1 monoclonal antibody. YS110 induces CD26 nuclear translocation through the caveolin pathway. YS110 inhibits the proliferation of tumor cell by delaying G2/M cell cycle transition. YS110 inhibits the infection of Middle East respiratory syndrome coronavirus (MERS CoV) by blocking the binding of MERS CoV S1 to CD26. YS110 can be used for researches on cancer or infection such as Malignant Mesothelioma and MERS.

Linagliptin-d₄ is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).

Sennidin B is an anthraquinone compound isolated from Cassia angustifolia. Sennidin B is a DPP-4 inhibitor with an IC₅₀ of 39.39 μM. Sennidin B is an insect chitinase inhibitor with a K_i of 80 nM against OfChi-h. Sennidin B competitively inhibits chitinase activity by forming π-π stacking interactions with key tryptophan residues in the active site through a folded conformation. Sennidin B activates PI3K/Akt to promote glucose uptake in adipocytes. Sennidin B can be used for the development of biopesticides and research on type 2 diabetes and metabolism-related signaling pathways.

Gemigliptin (LC15-0444 ) tartrate hydrate is a selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC₅₀ of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate hydrate exhibits potent anti-glycation properties. Gemigliptin tartrate hydrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

Sitagliptin-d₄ phosphate (MK-0431-d₄) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.

Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (K_i = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research.

Cichoriin is an orally active coumarin glycoside with broad biological activities. Cichoriin exhibits inhibitory activities against α-amylase, α-glucosidase, pancreatic lipase and DPP-IV, with IC₅₀ values of 5.76, 2.94, 16.83 and 9.16 μg/mL, respectively. Cichoriin significantly improves metabolic dysfunction-associated steatohepatitis (MASH) in mice by activating the AMPK signaling pathway. Cichoriin upregulates PPAR-γ in adipose tissue and alleviates obesity and associated cardiorenal injury in rats. Cichoriin blocks monosodium urate crystal-induced activation of the NLRP3 inflammasome and cell pyroptosis by inhibiting P2Y₁₄R (IC₅₀ = 8.47 nM). In silico virtual screening reveals that Cichoriin has a strong binding affinity for SARS-CoV-2.

Val-Pyrrolidide hydrochloride (compound 9) is a DPIV inhibitor. Val-Pyrrolidide hydrochloride can prevent N-terminal truncation of the peptide Gln3-Aβ(1–11)^[1].

Diprotin A TFA (Ile-Pro-Ile TFA) is an inhibitor of dipeptidyl peptidase IV (DPP-IV).