A DPP-4 inhibitor (IC50s = 0.37 and 0.29 nM for the human and rat enzymes

Teneligliptin (hydrobromide hydrate) – 50 mg

Brand:
Cayman
CAS:
1572583-29-9
Storage:
-20
UN-No:
Non-Hazardous - /

Teneligliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s = 0.37 and 0.29 nM for the human and rat enzymes, respectively).{46687} It is selective for DPP-4 over DPP-8 and DPP-9 (IC50s = 260 and 540 nM, respectively, for the human enzymes). Teneligliptin (0.03-1 mg/kg) inhibits increases in plasma glucose levels in an oral glucose tolerance test in Zucker fatty rats. It reduces body weight, inhibits hepatic steatosis, and decreases plasma insulin levels in a mouse model of high-fat diet-induced obesity when administered at doses of 30 and 60 mg/kg.{46688} Teneligliptin scavenges hydroxyl radicals in a cell-free assay (IC50 = 0.315 mM) and decreases urinary levels of 8-hydroxy-2′-deoxyguanosine (8-OHdG; Item No. 89320), a marker of oxidative stress, in a DPP-4-deficient rat model of diabetes induced by streptozotocin (STZ; Item No. 13104) when administered at a dose of 10 mg/kg per day.{46689}  

 

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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

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