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 SGLT抑制剂(11) 新SGLT产品

目录号	产品描述	文献引用	实验数据
S1548	Dapagliflozin Dapagliflozin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。	Cell Death Dis, 2019, 10(6):420 Front Pharmacol, 2019, 10:362 Nat Prod Bioprospect, 2019, 9(1):13-21	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 Canagliflozin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。	Cell Death Dis, 2019, 10(6):420 J Transl Med, 2019, 17(1):127 Front Pharmacol, 2019, 10:362	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。	Cell Death Dis, 2019, 10(6):420 Front Pharmacol, 2019, 10:362 Diabetes, 2016, 65(9):2784-94	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。
S8103	Sotagliflozin (LX4211) Sotagliflozin (LX4211)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。	J Cell Mol Med, 2018, 22(11):5367-5377 Vascul Pharmacol, 2018, 109:56-71
S8558	Tofogliflozin(CSG 452) Tofogliflozin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。
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 Phloretin 是一种二氢查尔酮，含有多元酚。	Oxid Med Cell Longev, 2019, 2019:2084805 J Agric Food Chem, 2017, 65(31):6625-6637	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 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。	Int J Biol Sci, 2019, 15(11):2497-2508 Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089 Nat Prod Bioprospect, 2019, 9(1):13-21	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).
S5413	Ertugliflozin Ertugliflozin 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.

目录号	产品描述	文献引用	实验数据
S1548	Dapagliflozin Dapagliflozin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。	Cell Death Dis,2019, 10(6):420 Front Pharmacol,2019, 10:362 Nat Prod Bioprospect,2019, 9(1):13-21	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 Canagliflozin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。	Cell Death Dis,2019, 10(6):420 J Transl Med,2019, 17(1):127 Front Pharmacol,2019, 10:362	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。	Cell Death Dis,2019, 10(6):420 Front Pharmacol,2019, 10:362 Diabetes,2016, 65(9):2784-94	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。
S8103	Sotagliflozin (LX4211) Sotagliflozin (LX4211)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。	J Cell Mol Med,2018, 22(11):5367-5377 Vascul Pharmacol,2018, 109:56-71
S8558	Tofogliflozin(CSG 452) Tofogliflozin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。
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 Phloretin 是一种二氢查尔酮，含有多元酚。	Oxid Med Cell Longev,2019, 2019:2084805 J Agric Food Chem,2017, 65(31):6625-6637	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 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。	Int J Biol Sci,2019, 15(11):2497-2508 Am J Physiol Renal Physiol,2019, 316(5):F1078-F1089 Nat Prod Bioprospect,2019, 9(1):13-21	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).
S5413	Ertugliflozin Ertugliflozin 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.