T-1095

T-1095 is a selective and orally active Na+-glucose cotransporter (SGLT) inhibitor with IC50s of 22.8 µM and 2.3 µM for human SGLT1 and SGLT2, respectively. T-1095 can be used for diabetes research[1].

Research Areas >> Metabolic Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> SGLT

hSGLT1:22.8 μM (IC50)

hSGLT2:2.3 μM (IC50)

T-1095 is absorbed into the circulation via oral administration, is metabolized to the active form, T-1095A, and suppresses the activity of SGLTs in the kidney[1]. Orally administered T-1095 (3-30 mg/kg) increases urinary glucose excretion in diabetic animals, thereby decreasing blood glucose levels[1]. With long-term T-1095 (0.01% or 0.1% T-1095 mixed diet; for 28 days) treatment, both blood glucose and HbA1c levels were reduced in streptozotocin (STZ)-induced diabetic rats and yellow KK mice. In addition, there was amelioration of abnormal carbohydrate metabolism, i.e., hyperinsulinemia and hypertriglyceridemia, and of the development of microalbuminuria, in yellow KK mice[1].

[1]. A Oku, et al. T-1095, an inhibitor of renal Na+-glucose cotransporters, may provide a novel approach to treating diabetes. Diabetes. 1999 Sep;48(9):1794-800.