Description
A DPP-4 inhibitor (IC50s = 0.37 and 0.29 nM for the human and rat enzymes, respectively); selective for DPP-4 over DPP-8 and DPP-9 (IC50s = 260 and 540 nM, respectively, for the human enzymes); inhibits increases in plasma glucose levels in an oral glucose tolerance test in Zucker fatty rats at 0.03-1 mg/kg; reduces body weight, inhibits hepatic steatosis, and decreases plasma insulin levels in a mouse model of high-fat diet-induced obesity at 30 and 60 mg/kg; scavenges hydroxyl radicals in a cell-free assay (IC50 = 0.315 mM); decreases urinary levels of 8-OHdG in a DPP-4-deficient rat model of STZ-induced diabetes at 10 mg/kg per day
Formal name: [(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]-3-thiazolidinyl-methanone, hydrobromide hydrate
Synonyms:
Molecular weight: 426.6
CAS: 1572583-29-9
Purity: ≥98%
Formulation: A crystalline solid
