tcsc0976 Ertugliflozin

Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC₅₀ of 0.877 nM for h-SGLT2^[1]. A drug for the treatment of type 2 diabetes mellitus^[2].

IC50 & Target: IC50: 0.877 nM (h-SGLT2)^[1].

In Vitro: Ertugliflozin (PF-04971729) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro^[3].

In Vivo: Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats^[3].