Dapagliflozin (BMS-512148): Selectivity & Specificity
Dapagliflozin (BMS-512148) is a potent inhibitor of SGLT-2 (1.6 ± 0.3 nM), SGLT2 (0.49 nM), SGLT1 (3.2 nM), SGLT3 (1.35 nM), SGLT6 (380 nM), Lox-1, ACAT1, ABCA1, STAT3, TLR4, NF-κB, hepcidin, ferritin, Kv channels, NHE1, NLRP3, AMPK, mTORC2, mTORC1, PAR2. Dapagliflozin (BMS-512148) exhibits the greatest inhibitory potency toward SGLT2 (IC50 = 0.49 nM).