linagliptin
Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output.
Ligand Summary
UNII: 3X29ZEJ4R2
PubChem: 10096344
Guide to Pharmacology: 6318
ChEMBL: CHEMBL237500
DrugCentral: 4175
LyCHI: VMG5TXYCPR3B
Target Activities
DPP4
Dipeptidyl peptidase 4
19 Activities
Items per page:
1 – 10 of 19
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Ki | 9 | |||||
IC50 | 10 | Bioorg. Med. Chem. Lett., (2012) 22:3:1464 | ||||
IC50 | 10 | ACS Med. Chem. Lett., (2016) 7:5:498 | ||||
IC50 | 9 | J. Med. Chem., (2007) 50:26:6450 | ||||
IC50 | 9 | Bioorg. Med. Chem. Lett., (2008) 18:11:3158 | ||||
IC50 | 9 | Bioorg. Med. Chem., (2012) 20:19:5864 | ||||
IC50 | 9 | Med Chem Res, (2013) 22:9:4505 | ||||
IC50 | 9 | Bioorg. Med. Chem., (2013) 21:11:2795 | ||||
IC50 | 9 | MedChemComm, (2014) 5:11:1700 | ||||
IC50 | 9 | None, (2016) None:None:None | ||||
FAP
Prolyl endopeptidase FAP
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.15 | ACS Med. Chem. Lett., (2016) 7:5:498 | ||||
IC50 | 7.05 | Bioorg. Med. Chem., (2012) 20:19:5864 | ||||
IC50 | 7.05 | MedChemComm, (2014) 5:11:1700 | ||||
IC50 | 6.43 | MedChemComm, (2014) 5:11:1700 | ||||
IC50 | 7.05 | |||||