Canagliflozin is an inhibitor of sodium-glucose cotransporter 2 (SGLT2; IC50 = 2.2 nM) that less potently blocks SGLT1 (IC50 = 910 nM).1 Canagliflozin is orally bioavailable and lowers plasma glucose by lowering the renal threshold for glucose and increasing urinary glucose excretion in animals.1,2 Formulations containing SGLT2 inhibitors, including canagliflozin, are used to treat type 2 diabetes mellitus.3
1.Nomura, S., Sakamaki, S., Hongu, M., et al.Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitusJ. Med. Chem.53(17)6355-6360(2010) 2.Sha, S., Devineni, D., Ghosh, A., et al.Canagliflozin, a novel inhibitor of sodium glucose co-transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjectsDiabetes Obes. Metab.13(7)669-672(2011) 3.Reed, J.W.Impact of sodium-glucose cotransporter 2 inhibitors on blood pressureVasc. Health Risk Manag.12393-405(2016)