Luseogliflozin (TS 071) is a potent, selective, orally active sodium-dependent glucose cotransporter (SGLT) 2 inhibitor, with an IC50 of 2.26 nM, about 1765-fold selectivity over SGLT1 (IC50, 3990 nM). Luseogliflozin has the protential for researching type 2 diabetes.
Luseogliflozin competitively inhibits the sodium-dependent uptake of 14C-α-metlglucoside by Chinese hamster ovary K1 cells overexpressing human SGLT2 in vitro (Ki value 1.10 nM)[1].Luseogliflozin (20% OSI-096 and Luseogliflozin-generated serum, 24 h) induces β-cell proliferation through a humoral factor-mediated FoxM1/PLK1/CENP-A pathway independent of insulin signaling[2].
Luseogliflozin (10 mg/kg, oral, 7 days) improves perglycemia and promotes β-cell proliferation in mice[2].
References:
[1]. Anthony Markham,et al. Luseogliflozin: first global approval. Drugs. 2014 Jun;74(8):945-50.
[2]. Jun Shirakawa,et al. Luseogliflozin increases beta cell proliferation through humoral factors that activate an insulin receptor- and IGF-1 receptor-independent pathway. Diabetologia. 2020 Mar;63(3):577-587.