| s5566 |
Dapagliflozin propanediol monohydrate |
Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors. |
Selective |
|
| S4431 |
Ertugliflozin L-pyroglutamic acid |
Ertugliflozin (MK-8835, PF-04971729) L-pyroglutamic acid is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2) with IC50 of 0.877 nM for h-SGLT2. Ertugliflozin has the potential for the treatment of type 2 diabetes mellitus. |
Selective |
h-SGLT2, IC50: 0.877 nM |
| S5413 |
Ertugliflozin |
Ertugliflozin (MK-8835, PF-04971729) is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1. |
Selective |
hSGLT2, IC50: 0.877 nM |
| S1548 |
Dapagliflozin |
Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4. |
Selective |
hSGLT2, EC50: 1.1 nM |
| S8103 |
Sotagliflozin |
Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.
|
Selective |
SGLT2, IC50: 1.8 nM |
| S5901 |
Canagliflozin hemihydrate |
Canagliflozin hemihydrate is the hemihydrate form of canagliflozin, which is a SGLT2 inhibitor with IC50 of 2.2 nM for hSGLT2 in a cell-free assay, exhibits 413-fold selectivity over hSGLT1. |
Selective |
mSGLT2, IC50: 2 nM; hSGLT2, IC50: 4.4 nM |
| S2760 |
Canagliflozin (JNJ 28431754) |
Canagliflozin (TA 7284, JNJ 28431754) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1. |
Selective |
hSGLT2, IC50: 4.4 nM; rSGLT2, IC50: 3.7 nM; mSGLT2, IC50: 2 nM |
| S8558 |
Tofogliflozin(CSG 452) |
Tofogliflozin (CSG 452) is a novel sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and hSGLT1, respectively.
|
Selective |
hSGLT2, IC50: 2.9 nM |
| S8022 |
Empagliflozin |
Empagliflozin is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3. |
Selective |
SGLT2, IC50: 3.1 nM |
| S8637 |
Ipragliflozin (ASP1941) |
Ipragliflozin (ASP1941) is a highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor with an IC50 value of 7.4 nM for hSGLT2 and a 254-fold selectivity versus SGLT1.
|
Selective |
hSGLT2, IC50: 7.4 nM; rat SGLT2, IC50: 6.73 nM; mouse SGLT2, IC50: 5.64 nM |
| S0994 |
Ipragliflozin L-Proline |
Ipragliflozin L-Proline is an orally active and selective inhibitor of SGLT2 with IC50 of 7.38 nM, 6.73 nM and 5.64 nM for human SGLT2, rat SGLT2 and mouse SGLT2, respectively. |
Selective |
human SGLT2, IC50: 7.38 nM; rat SGLT2, IC50: 6.73 nM; mouse SGLT2, IC50: 5.64 nM |
| S2343 |
Phlorizin |
Phlorizin (Phloridzin) is a dihydrochalcone found in the bark of pear (Pyrus communis), apple, cherry and other fruit trees. Phlorizin is a non-selective SGLT inhibitor with Ki of 300 nM and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor. |
Pan |
hSGLT2, Ki: 39 nM |
| S2342 |
Phloretin (RJC 02792) |
Phloretin (RJC 02792, NSC 407292, Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes. |
Pan |
|