DBPR108

DBPR108 is an inhibitor of dipeptidyl peptidase 4 (DPP-4; IC₅₀ = 0.015 µM).¹ It is selective for DPP-4 over DPP-8 and DPP-9 (IC₅₀s = >50 µM for both). DBPR108 (10 mg/kg) increases plasma levels of glucagon-like peptide 1 (GLP-1) and insulin in rats.² It reduces blood glucose levels in an oral glucose tolerance test in mice when administered at a dose of 3 mg/kg.¹ DBPR108 (0.1 mg/kg), alone and in combination with the biguanide metformin (Item No. 13118), decreases blood glucose levels in an oral glucose tolerance test in a mouse model of high-fat diet-induced obesity.²

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1. Yeh, T.-K., Tsai, T.-Y., Hsu, T., et al. (2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: A potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. Bioorg. Med. Chem. Lett. 20(12), 3596-3600 (2010).

2. Yeh, K.-C., Yeh, T.-K., Huang, C.-Y., et al. DBPR108, a novel dipeptidyl peptidase-4 inhibitor with antihyperglycemic activity. Life Sci. 278, 119574 (2021).