SGLT

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研究领域

抑制剂选择性比较

特异性亚型抑制剂

SGLT产品

所有产品(17) SGLT抑制剂(17)

目录号	产品描述	文献引用	实验数据
S1548	Dapagliflozin (BMS-512148) Dapagliflozin (BMS-512148) 是一种有效的，选择性的hSGLT2抑制剂，EC50为1.1 nM，比作用于hSGLT1选择性高1200倍。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)是一种高效的，选择性SGLT2抑制剂，作用于hSGLT2，无细胞试验中IC50为2.2 nM，比作用于hSGLT1选择性高413倍。	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Hypertension, 2021, 77(2):729-738 Int J Mol Sci, 2021, 22(15)7774	Canagliflozin dose-dependently increases pAMPK and pACC in PC3 cells after 30 min
S8022	Empagliflozin (BI 10773) Empagliflozin (BI 10773)是一种有效的，选择性SGLT-2抑制剂，IC50为3.1 nM，比作用于SGLT-1， 4， 5和6选择性高300倍以上。Phase 3。	Cardiovasc Diabetol, 2022, 21(1):27 Int J Mol Sci, 2021, 22(10)5089 Redox Biol, 2020, 2;32:101527	Effects of empagliflozin on AMPK/ACC phosphorylation
S5901	Canagliflozin hemihydrate Canagliflozin hemihydrate是canagliflozin的半水化合物形式。Canagliflozin是SGLT2的抑制剂，对hSGLT2的IC50值为2.2 nM，对hSGLT2的选择性是对hSGLT1的413倍。	Cell Death Dis, 2018, 9(2):226
S8103	Sotagliflozin (LX4211) Sotagliflozin (LX4211, LP-802034)是一种口服的双重SGLT1/SGLT2抑制剂，IC50分别为 36 nM 和 1.8 nM。Phase 3。	Mol Ther Methods Clin Dev, 2022, 24:11-19 Cell Rep, 2021, 36(12):109742 Cancer Lett, 2021, 519:277-288
E0141^New	Bexagliflozin (EGT1442) Bexagliflozin (EGT1442, EGT-0001442, THR-1442) 是一种有效的选择性 SGLT2 抑制剂，IC50 为 2 nM。
S8558	Tofogliflozin(CSG 452) Tofogliflozin (CSG 452) 是一种新型的sodium-glucose co-transporter 2(SGLT2)抑制剂，对hSGLT2和hSGLT1的IC50值分别为2.9 nM和8444 nM。
S0993	Remogliflozin etabonate (GSK189075) Remogliflozin etabonate (GSK189075) 是一种口服活性的、选择性和低亲和力的 sodium glucose cotransporter (SGLT2) 的抑制剂，对应hSGLT2、rSGLT2、hSGLT1 和 rSGLT1 的Ki值分别为1950 nM、2140 nM、43100 nM和8570 nM。Remogliflozin etabonate 在啮齿动物模型中显示出抗糖尿病的功效。
S0994	Ipragliflozin L-Proline Ipragliflozin L-Proline 是一种口服活性的 SGLT2 的选择性抑制剂，对人SGLT2、大鼠SGLT2和小鼠SGLT2的IC50分别为7.38 nM、6.73 nM和5.64 nM。
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)是一种高度选择性的sodium-glucose cotransporter 2 (SGLT2)抑制剂，对hSGLT2的IC50值为7.4 nM，对SGLT2的选择性是对SGLT1的选择性的254倍。
S2342	Phloretin (RJC 02792) Phloretin (RJC 02792, NSC 407292, Dihydronaringenin)是一种二氢查尔酮，含有多元酚。	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) 是有毒的2'-葡萄糖苷根皮素，属于二氢查尔酮，是一种黄酮类化合物。Phlorizin 是一种非选择性的 SGLT 的抑制剂，对hSGLT1 和 hSGLT2的Ki值分别为300 nM 和 39 nM。Phlorizin 也是 Na+/K+-ATPase 的抑制剂。	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是一种有效、选择性的、高亲和力的 sodium glucose cotransporter 1 (SGLT1) 抑制剂，对human SGLT1和rat SGLT1的Ki值分别为97.4 nM和43.5 nM。KGA-2727的选择性比(Ki for SGLT2/Ki for SGLT1)为140 (human)和390 (rat)。 KGA-2727在啮齿动物模型中显示出抗糖尿病功效。
S8939	Mizagliflozin (KWA 0711) Mizagliflozin (KWA 0711)是一种新型、有效、选择性的 sodium glucose co-transporter 1 (SGLT1) 抑制剂，对human SGLT1的Ki值为27 nM。Mizagliflozin的选择性比(Ki value for human SGLT2/Ki value for human SGLT1)为303。Mizagliflozin还有改善慢性便秘的潜在应用。
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 是一种有效的、选择性的 sodium-dependent glucose cotransporter 2 (SGLT2) 的口服活性抑制剂，对h-SGLT2的IC50值为0.877 nM。Ertugliflozin 具有治疗2型糖尿病的潜力。

目录号	产品描述	文献引用	实验数据
S1548	Dapagliflozin (BMS-512148) Dapagliflozin (BMS-512148) 是一种有效的，选择性的hSGLT2抑制剂，EC50为1.1 nM，比作用于hSGLT1选择性高1200倍。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)是一种高效的，选择性SGLT2抑制剂，作用于hSGLT2，无细胞试验中IC50为2.2 nM，比作用于hSGLT1选择性高413倍。	Nat Chem Biol,2022, 10.1038/s41589-022-00996-7 Hypertension,2021, 77(2):729-738 Int J Mol Sci,2021, 22(15)7774	Canagliflozin dose-dependently increases pAMPK and pACC in PC3 cells after 30 min
S8022	Empagliflozin (BI 10773) Empagliflozin (BI 10773)是一种有效的，选择性SGLT-2抑制剂，IC50为3.1 nM，比作用于SGLT-1， 4， 5和6选择性高300倍以上。Phase 3。	Cardiovasc Diabetol,2022, 21(1):27 Int J Mol Sci,2021, 22(10)5089 Redox Biol,2020, 2;32:101527	Effects of empagliflozin on AMPK/ACC phosphorylation
S5901	Canagliflozin hemihydrate Canagliflozin hemihydrate是canagliflozin的半水化合物形式。Canagliflozin是SGLT2的抑制剂，对hSGLT2的IC50值为2.2 nM，对hSGLT2的选择性是对hSGLT1的413倍。	Cell Death Dis,2018, 9(2):226
S8103	Sotagliflozin (LX4211) Sotagliflozin (LX4211, LP-802034)是一种口服的双重SGLT1/SGLT2抑制剂，IC50分别为 36 nM 和 1.8 nM。Phase 3。	Mol Ther Methods Clin Dev,2022, 24:11-19 Cell Rep,2021, 36(12):109742 Cancer Lett,2021, 519:277-288
E0141^New	Bexagliflozin (EGT1442) Bexagliflozin (EGT1442, EGT-0001442, THR-1442) 是一种有效的选择性 SGLT2 抑制剂，IC50 为 2 nM。
S8558	Tofogliflozin(CSG 452) Tofogliflozin (CSG 452) 是一种新型的sodium-glucose co-transporter 2(SGLT2)抑制剂，对hSGLT2和hSGLT1的IC50值分别为2.9 nM和8444 nM。
S0993	Remogliflozin etabonate (GSK189075) Remogliflozin etabonate (GSK189075) 是一种口服活性的、选择性和低亲和力的 sodium glucose cotransporter (SGLT2) 的抑制剂，对应hSGLT2、rSGLT2、hSGLT1 和 rSGLT1 的Ki值分别为1950 nM、2140 nM、43100 nM和8570 nM。Remogliflozin etabonate 在啮齿动物模型中显示出抗糖尿病的功效。
S0994	Ipragliflozin L-Proline Ipragliflozin L-Proline 是一种口服活性的 SGLT2 的选择性抑制剂，对人SGLT2、大鼠SGLT2和小鼠SGLT2的IC50分别为7.38 nM、6.73 nM和5.64 nM。
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)是一种高度选择性的sodium-glucose cotransporter 2 (SGLT2)抑制剂，对hSGLT2的IC50值为7.4 nM，对SGLT2的选择性是对SGLT1的选择性的254倍。
S2342	Phloretin (RJC 02792) Phloretin (RJC 02792, NSC 407292, Dihydronaringenin)是一种二氢查尔酮，含有多元酚。	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) 是有毒的2'-葡萄糖苷根皮素，属于二氢查尔酮，是一种黄酮类化合物。Phlorizin 是一种非选择性的 SGLT 的抑制剂，对hSGLT1 和 hSGLT2的Ki值分别为300 nM 和 39 nM。Phlorizin 也是 Na+/K+-ATPase 的抑制剂。	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是一种有效、选择性的、高亲和力的 sodium glucose cotransporter 1 (SGLT1) 抑制剂，对human SGLT1和rat SGLT1的Ki值分别为97.4 nM和43.5 nM。KGA-2727的选择性比(Ki for SGLT2/Ki for SGLT1)为140 (human)和390 (rat)。 KGA-2727在啮齿动物模型中显示出抗糖尿病功效。
S8939	Mizagliflozin (KWA 0711) Mizagliflozin (KWA 0711)是一种新型、有效、选择性的 sodium glucose co-transporter 1 (SGLT1) 抑制剂，对human SGLT1的Ki值为27 nM。Mizagliflozin的选择性比(Ki value for human SGLT2/Ki value for human SGLT1)为303。Mizagliflozin还有改善慢性便秘的潜在应用。
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 是一种有效的、选择性的 sodium-dependent glucose cotransporter 2 (SGLT2) 的口服活性抑制剂，对h-SGLT2的IC50值为0.877 nM。Ertugliflozin 具有治疗2型糖尿病的潜力。