O-desethyl Dapagliflozin is an inhibitor of sodium-glucose cotransporter 2 (SGLT2; IC50 = 9.4 nM) and active metabolite of dapagliflozin .1,2 It is selective for SGLT2 over SGLT1 (IC50 = 970 nM).1
1.Xu, B., Feng, Y., Cheng, H., et al.C-aryl glucosides substituted at the 4’-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetesBioorg. Med. Chem. Lett.21(15)4465-4470(2011) 2.Xu, G., Lv, B., Roberge, J.Y., et al.Design, synthesis, and biological evaluation of deuterated C-aryl glycoside as a potent and long-acting renal sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetesJ. Med. Chem.57(4)1236-1251(2014)