Luseogliflozin (TS 071) hydrate, a second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor, exhibits selective potency and oral activity, with an IC50 of 2.26 nM. This compound is utilized in research for the treatment of type 2 diabetes mellitus (T2DM).

SGLT2:2.26 nM (IC50)

Luseogliflozin can increase beta cell proliferation through the activation of the FoxM1/PLK1/CENP-A pathway via humoral factors thats act in an insulin/IGF-1 receptor-independent manner. Luseogliflozin increases beta cell proliferation in OSI-906-treated mice[2]. Cell Viability Assay[2]Cell Line: βIRKO, IRS1KO and IRS2KO beta cells Concentration: 100 nM Incubation Time: 24 and 48 hours Result: Cell Viability Assay[2]Treating cells with serum from the OSI-906 (200 nM) or OSI-906+Luseogliflozin(100 nM) group led to significantly increased cell viability in the latter group in the control, IRS1KO, IRS2KO, as well as the insulin receptor (IR)-deficient βIRKO beta cells.

SGLT2 inhibition with Luseogliflozin (10 mg/kg/daily; oral gavage) significantly ameliorates hyperglycaemia, but not hyperinsulinaemia, in the OSI-906(45 mg/kg)-treated mice. Luseogliflozin ameliorates hyperglycaemia induced by OSI-906[2]. Animal Model: C57BL/6J male mice aged 8 weeks old[2]Dosage: 10 mg/kg/daily Administration: Oral gavage; for 7 days between 08:00 and 09:00 hours Result: Treatment significantly ameliorated the OSI-906 (45 mg/kg)-induced hyperglycaemia.