SGLT

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1548	Dapagliflozin (BMS-512148)	<1 mg/mL	82 mg/mL	''17 mg/mL
S2760	Canagliflozin (JNJ 28431754)	<1 mg/mL	88 mg/mL	'<1 mg/mL
S8022	Empagliflozin (BI 10773)	<1 mg/mL	90 mg/mL	<1 mg/mL
S8103	Sotagliflozin (LX4211)	<1 mg/mL	84 mg/mL	'17 mg/mL
S8558	Tofogliflozin(CSG 452)	4 mg/mL	84 mg/mL	84 mg/mL
E0141	Bexagliflozin (EGT1442)	93 mg/mL	93 mg/mL	23 mg/mL
S0993	Remogliflozin etabonate (GSK189075)	<1 mg/mL	100 mg/mL	''''25 mg/mL
S0994	Ipragliflozin L-Proline	<1 mg/mL	35 mg/mL	6 mg/mL
S5566	Dapagliflozin propanediol monohydrate	<1 mg/mL	100 mg/mL	100 mg/mL
S8637	Ipragliflozin (ASP1941)	<1 mg/mL	80 mg/mL	80 mg/mL
S2342	Phloretin (RJC 02792)	<1 mg/mL	54 mg/mL	54 mg/mL
S2343	Phlorizin	<1 mg/mL	87 mg/mL	9 mg/mL
S8938	KGA-2727	100 mg/mL	100 mg/mL	45 mg/mL
S8939	Mizagliflozin (KWA 0711)	100 mg/mL	100 mg/mL	''100 mg/mL
S5413	Ertugliflozin	87 mg/mL	87 mg/mL	87 mg/mL
S4431	Ertugliflozin L-pyroglutamic acid	10 mg/mL	100 mg/mL	''100 mg/mL

亜型選択性的な製品

SGLT製品

All (16) SGLT阻害剤(16)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1548	Dapagliflozin (BMS-512148) Dapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.	Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00885-8 Cell Cycle, 2022, 1-14 PLoS One, 2022, 17(2):e0258054	Effects of once-daily administration of DAPA, DAPA switched to (DAla2)GIP or saline vehicle on (AeD) DEXA images, (E) body fat, (F) lean mass, (G) bone mineral content and (H) bone mineral density in high fat fed mice. Mice received saline vehicle (0.9% wt/vol; po), DAPA (1 mg/kg; po) once-daily over 28 days, or DAPA (1 mg/kg; po) once-daily over 14 days followed by (DAla2)GIP (25 nmol/kg; ip) once-daily for 14 days. Lean control mice received saline vehicle once-daily. White bars=lean controls; grey bars=HF controls; black bars=DAPA; and hatched bars=DAPA / GIP. Values are mean ± SEM for groups of 6-8 mice. p < 0.05 and *p < 0.01 compared to HF controls.
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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Cell Mol Life Sci, 2022, 79(5):273 Cell Death Dis, 2022, 13(6):523	Canagliflozin dose-dependently increases pAMPK and pACC in PC3 cells after 30 min
S8022	Empagliflozin (BI 10773) Empagliflozin (BI-10773) 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.	Cell Mol Life Sci, 2022, 79(5):273 Cardiovasc Diabetol, 2022, 21(1):27 Cardiol J, 2022, 10.5603/CJ.a2022.0033	Effects of empagliflozin on AMPK/ACC phosphorylation
S8103	Sotagliflozin (LX4211) Sotagliflozin (LX4211, LP-802034) is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.	Mol Ther Methods Clin Dev, 2022, 24:11-19 Cell Rep, 2021, 36(12):109742 Cancer Lett, 2021, 519:277-288
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.
E0141^新	Bexagliflozin (EGT1442) Bexagliflozin (EGT1442, EGT-0001442, THR-1442) is a potent and selective SGLT2 inhibitor with an IC50 of 2 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.
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.
S5566	Dapagliflozin propanediol monohydrate Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors.	Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089
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.
S2342	Phloretin (RJC 02792) Phloretin (RJC 02792, NSC 407292, Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes.	Food Funct, 2020, 10.1039/d0fo02362k Oxid Med Cell Longev, 2019, 2019:2084805 J Med Virol, 2019, 91(8):1440-1447	Specificity of FDG uptake in BJAB, OCI-LY3 and SU-DHL-6 cells. Cells were incubated without inhibitors or with 2 mM 2-DG, 5 μM cytochalasin B or 10 μM phloretin for 24 h or with 50 μM CoCl2 for 30 min and 100 kBq of FDG for 30 min. Cell-bound radioactivity was normalized to protein concentration determined from a parallel sample and expressed as % of untreated control, mean ± standard deviation from fourfold determinations; Asterisks indicates significant decrease or increase (p < 0.05, Student’s t test)
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.	Mol Ther Methods Clin Dev, 2022, 24:11-19 Int J Biol Sci, 2019, 15(11):2497-2508 Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089	PQ increases glucose transport and the translocation of glucose transporters. Cells were treated with PQ for 48 h. The survival of cells treated with PQ in the presence or absence of phlorizin (e) was determined. Bar graph represents percents of viable cells (cell survival).
S8938	KGA-2727 KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.
S8939	Mizagliflozin (KWA 0711) Mizagliflozin (KWA 0711) is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation.
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.
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.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1548	Dapagliflozin (BMS-512148) Dapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.	Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00885-8 Cell Cycle, 2022, 1-14 PLoS One, 2022, 17(2):e0258054	Effects of once-daily administration of DAPA, DAPA switched to (DAla2)GIP or saline vehicle on (AeD) DEXA images, (E) body fat, (F) lean mass, (G) bone mineral content and (H) bone mineral density in high fat fed mice. Mice received saline vehicle (0.9% wt/vol; po), DAPA (1 mg/kg; po) once-daily over 28 days, or DAPA (1 mg/kg; po) once-daily over 14 days followed by (DAla2)GIP (25 nmol/kg; ip) once-daily for 14 days. Lean control mice received saline vehicle once-daily. White bars=lean controls; grey bars=HF controls; black bars=DAPA; and hatched bars=DAPA / GIP. Values are mean ± SEM for groups of 6-8 mice. p < 0.05 and *p < 0.01 compared to HF controls.
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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Cell Mol Life Sci, 2022, 79(5):273 Cell Death Dis, 2022, 13(6):523	Canagliflozin dose-dependently increases pAMPK and pACC in PC3 cells after 30 min
S8022	Empagliflozin (BI 10773) Empagliflozin (BI-10773) 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.	Cell Mol Life Sci, 2022, 79(5):273 Cardiovasc Diabetol, 2022, 21(1):27 Cardiol J, 2022, 10.5603/CJ.a2022.0033	Effects of empagliflozin on AMPK/ACC phosphorylation
S8103	Sotagliflozin (LX4211) Sotagliflozin (LX4211, LP-802034) is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.	Mol Ther Methods Clin Dev, 2022, 24:11-19 Cell Rep, 2021, 36(12):109742 Cancer Lett, 2021, 519:277-288
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.
E0141^新	Bexagliflozin (EGT1442) Bexagliflozin (EGT1442, EGT-0001442, THR-1442) is a potent and selective SGLT2 inhibitor with an IC50 of 2 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.
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.
S5566	Dapagliflozin propanediol monohydrate Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors.	Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089
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.
S2342	Phloretin (RJC 02792) Phloretin (RJC 02792, NSC 407292, Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes.	Food Funct, 2020, 10.1039/d0fo02362k Oxid Med Cell Longev, 2019, 2019:2084805 J Med Virol, 2019, 91(8):1440-1447	Specificity of FDG uptake in BJAB, OCI-LY3 and SU-DHL-6 cells. Cells were incubated without inhibitors or with 2 mM 2-DG, 5 μM cytochalasin B or 10 μM phloretin for 24 h or with 50 μM CoCl2 for 30 min and 100 kBq of FDG for 30 min. Cell-bound radioactivity was normalized to protein concentration determined from a parallel sample and expressed as % of untreated control, mean ± standard deviation from fourfold determinations; Asterisks indicates significant decrease or increase (p < 0.05, Student’s t test)
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.	Mol Ther Methods Clin Dev, 2022, 24:11-19 Int J Biol Sci, 2019, 15(11):2497-2508 Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089	PQ increases glucose transport and the translocation of glucose transporters. Cells were treated with PQ for 48 h. The survival of cells treated with PQ in the presence or absence of phlorizin (e) was determined. Bar graph represents percents of viable cells (cell survival).
S8938	KGA-2727 KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.
S8939	Mizagliflozin (KWA 0711) Mizagliflozin (KWA 0711) is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation.
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.
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.

Tags: SGLT inhibitor|SGLT agonist|SGLT activator|SGLT inducer|SGLT antagonist|SGLT signaling pathway|SGLT assay kit