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SGLT2 選択性 阻害剤

製品コード 製品名 製品説明 Selective / Pan IC50 / Ki
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
S0993 Remogliflozin etabonate (GSK189075) Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models. Selective hSGLT2, Ki: 1950 nM; rSGLT2, Ki: 2140 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