Formulation: A solid
Formal Name: 1-[(2S)-2-amino-4-[5,8-dihydro-2,4-bis(trifluoromethyl)pyrido[3,4-d]pyrimidin-7(6H)-yl]-4-oxobutyl]-5,5-difluoro-2-piperidinone, (2R,3R)-2,3-dihydroxybutanedioate
Purity: ≥98%
Formula Markup: C18H19F8N5O2 • XC4H6O6
Formula Weight: 489,4
Shelf life (days): 1460
CAS Number: 1374639-74-3
Notes: Gemigliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 0.01 µM).{65325} It is selective for DPP-4 over DPP-8, DPP-9, and fibroblast activation protein-α (FAP-α; IC50s = 277.28, 233.72, 418.43 µM, respectively). Gemigliptin inhibits DPP-4 activity in isolated human, rat, dog, and monkey plasma (IC50s = 11.5, 14.5, 14.5, and 14 nM, respectively). It scavenges methylglyoxal in vitro and inhibits advanced glycation end product (AGE) formation between BSA and methylglyoxal and cross-linking of AGE-BSA with rat tail tendon collagen (IC50s = 1.15, 11.69, and 1.39 mM, respectively).{65324} Gemigliptin (100 mg/kg) reduces the levels of circulating AGE and red blood cell IgG content in a db/db mouse model of diabetes when administered for 12 weeks. It decreases blood glucose and hemoglobin A1c (HbA1c) levels and reduces pancreatic β-cell damage in a dose-dependent manner in a mouse model of diabetes induced by a high-fat diet and streptozotocin (STZ; Item No. 13104).{65325} Gemigliptin also induces cytotoxicity in SW1736 and TPC-1 human thyroid cancer cells.{65326,65327} Formulations containing gemigliptin have been used in the treatment of type 2 diabetes.
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