Bexagliflozin

Bexagliflozin (EGT1442) is an orally active and selective SGLT2 inhibitor with IC₅₀ values of 0.002 μM and 5.6 μM for SGLT2 and SGLT1, respectively. Bexagliflozin selectively inhibits SGLT2-mediated sodium-dependent glucose uptake. Bexagliflozin induces saturable urinary glucose excretion in normal rats and dogs. Bexagliflozin reduces blood glucose and HbA_1c levels in db/db mice without affecting body mass or insulin level. Bexagliflozin can be used for the research of type 2 diabetes mellitus, hypertensive stroke^[1]. In Vitro:Bexagliflozin (EGT1442) potently and selectively inhibits human SGLT2 with an IC₅₀ of 2 nM and 2435-fold selectivity over human SGLT1 in cell-based AMG uptake assays^[1]. In Vivo:Bexagliflozin (0.1-10 mg/kg; p.o.; single dose) dose-dependently reduces blood glucose AUC_0-t and increases urinary glucose excretion in normal Sprague-Dawley rats, with an ED₅₀ of 0.38 mg/kg for urinary glucose excretion^[1].
Bexagliflozin (0.03-3 mg/kg; p.o.; single dose) reduces post-glucose challenge blood glucose and induces dose-dependent urinary glucose excretion in normal beagle dogs, with an ED₅₀ of 0.09 mg/kg for urinary glucose excretion^[1].
Bexagliflozin (0.1-3 mg/kg; p.o.; daily; 30 days) dose-dependently reduces non-fasting blood glucose and HbA₁c levels, and improves oral glucose tolerance in db/db mice over 30 days of daily oral administration, without affecting plasma insulin or body weight^[1].
Bexagliflozin (3.0 mg/kg; p.o.; daily via drinking water; up to 2 months) significantly prolongs median survival by approximately 67% (from 32 to 53 days) in SHRSP rats fed a stroke-promoting high-salt diet^[1].