Canagliflozin D4

Canagliflozin-d₄ is intended for use as an internal standard for the quantification of canagliflozin by GC- or LC-MS. 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, have been 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)