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Empagliflozin is a selective inhibitor of SGLT-2 with IC50 value of 3.1 nM [1].

Sodium glucose cotransporter-2 (SGLT-2) is a member of sodium glucose co-transporter family and plays a pivotal role in glucose reabsorption in the kidney [2].

Empagliflozin is a potent SGLT-2 inhibitor and has a high degree of selectivity over SGLT-1, 4, 5 and 6 than other reported SGLT-2 inhibitors. When tested with a panel of human cell lines over-expressed SGLT-1, 2, 4, 5 and 6, Empagliflozin treatment competitively bind to SGLT-2 over glucose at low dose [1]. In human proximal tublular cell (PTC) cell line HK2 cells, Empagliflozin treatment for 72 h inhibits the expression of SGLT-2 which in turn reversed high glucose induced TLR4 expression, NF-κB binding, IL-6 secretion, AP-1 binding and CIV expression [3].

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