Bexagliflozin

Description: Bexagliflozin, formerly known as EGT1442, is a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. The IC(50) values for EGT1442 against human SGLT1 and SGLT2 are 5.6uM and 2nM, respectively. In normal rats and dogs a saturable urinary glucose excretion was produced with an ED(50) of 0.38 and 0.09mg/kg, respectively. EGT1442 showed favorable properties both in vitro and in vivo and could be beneficial to the management of type 2 diabetic patients.

References: Zhang W, Welihinda A, Mechanic J, Ding H, Zhu L, Lu Y, Deng Z, Sheng Z, Lv B, Chen Y, Roberge JY, Seed B, Wang YX. EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. Pharmacol Res. 2011 Apr; 63(4):284-93. doi: 10.1016/j.phrs.2011.01.001. Epub 2011 Jan 5. PubMed PMID: 21215314.