fluoro-Dapagliflozin

Dapagliflozin (Item No. 11574) is a selective sodium-glucose cotransporter (SGLT) inhibitor that blocks glucose transport with about 100-fold selectivity for SGLT2 (Ki = 6 nM; EC50 = 1.1 nM) over SGLT1 (Ki = 390 nM).{20895,20896} It improves glucose tolerance in normal rats and reduces hyperglycemia in Zucker diabetic fatty rats.{22762}fluoro-Dapagliflozin is an analog of dapagliflozin that displays similar selectivity for inhibiting SGLT2 over SGLT1 (Kis = 5.3 and 330 nM, respectively).{20895} fluoro-Dapagliflozin (10 nM) significantly reduces phlorizin-sensitive sugar transport in COS-1 cells expressing human SGLT2.{20895}