Phloretin (NSC-407292) is a well-known inhibitor of eukaryotic urea transporters, blocks VacA-mediated urea and ion transport. Phloretin is a dihydrochalcone, a type of natural phenols. It can be found in apple tree leaves and the Manchurian apricot. It promotes potent antioxidative activities in peroxynitrite scavenging and the inhibition of lipid peroxidation. It has been found to inhibit the growth of several cancer cells and induce apoptosis of B16 melanoma and HL60 human leukemia cells.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2), in development for treating type 2 diabetes mellitus (T2DM). It inhibits SGLT2, responsible for at least 90% of glucose reabsorption in the kidney.

PF-04971729 (Ertugliflozin (PF-04971729)) is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2).

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific inhibitor of SGLT2, with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2, respectively.

Phlorizin (Phloridzin) is a non-selective SGLT inhibitor found in apple, for hSGLT1( Ki=300 nM) and hSGLT2( Ki=39 nM) .

Empagliflozin (BI 10773) is an SGLT-2 inhibitor (IC50=3.1 nM) that is potent and selective, with more than 300-fold selectivity for SGLT-1/4/5/6. Empagliflozin is used for the treatment of type 2 diabetes.

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a selective and orally active hSGLT2 inhibitor with an IC50 of 0.877 nM, suitable for studies on the treatment of type 2 diabetes mellitus.