Tofogliflozin

Description: Tofogliflozin (also known as CSG-452) hydrate is a novel, very potent and highly selective inhibitor of sodium/glucose cotransporter 2 (SGLT2) with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse respectively. Tofogliflozin competitively inhibited SGLT2 in cells that overexpress SGLT2. The selectivity of tofogliflozin towards human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 is the highest among the tested SGLT2 inhibitors under clinical trials. Long-term inhibition of renal SGLT2 by tofogliflozin not only preserved pancreatic beta-cell function, but also prevented kidney dysfunction in a mouse model of type 2 diabetes. These findings suggest that long-term use of tofogliflozin in patients with type 2 diabetes may prevent progression of diabetic nephropathy.

References: J Pharmacol Exp Ther. 2012 Jun; 341(3):692-701.

Related CAS#:1201913-82-7 (hydrate)