Teneligliptin (hydrobromide hydrate)

Teneligliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor (IC₅₀s = 0.37 and 0.29 nM for the human and rat enzymes, respectively).¹ 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.² 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.³

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1. Yoshida, T., Akahoshi, F., Sakashita, H., et al. Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): A highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg. Med. Chem. 20(19), 5705-5719 (2012).

2. Fukuda-Tsuru, S., Kakimoto, T., Utsumi, H., et al. The novel dipeptidyl peptidase-4 inhibitor teneligliptin prevents high-fat diet-induced obesity accompanied with increased energy expenditure in mice. Eur. J. Pharmacol. 723, 207-215 (2014).

3. Kimura, S., Inoguchi, T., Yamasaki, T., et al. A novel DPP-4 inhibitor teneligliptin scavenges hydroxyl radicals: In vitro study evaluated by electron spin resonance spectroscopy and in vivo study using DPP-4 deficient rats. Metabolism 65(3), 138-145 (2016).