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) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1548 | Dapagliflozin | <1 mg/mL | 82 mg/mL | 17 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 |
| S0994 | Ipragliflozin L-Proline | <1 mg/mL | 35 mg/mL | 6 mg/mL |
| S8938 | KGA-2727 | 100 mg/mL | 100 mg/mL | 45 mg/mL |
| S8939 | Mizagliflozin | 100 mg/mL | 100 mg/mL | '100 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 | <1 mg/mL | 54 mg/mL | 54 mg/mL |
| S2343 | Phlorizin | <1 mg/mL | 87 mg/mL | 9 mg/mL |
| S5413 | Ertugliflozin | 87 mg/mL | 87 mg/mL | 87 mg/mL |
亜型選択性的な製品
SGLT製品
| 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 |
DapagliflozinDapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4. |
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. |
|
| 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. |
Effects of empagliflozin on AMPK/ACC phosphorylation
|
|
| S8103 |
Sotagliflozin (LX4211)Sotagliflozin (LX4211) is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3. |
||
| 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. |
||
| S0994新 |
Ipragliflozin L-ProlineIpragliflozin 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. |
||
| S8938新 |
KGA-2727KGA-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新 |
MizagliflozinMizagliflozin (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. |
||
| S5566 |
Dapagliflozin propanediol monohydrateDapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors. |
||
| 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 |
PhloretinPhloretin (Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes. |
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 |
PhlorizinPhlorizin (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. |
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 |
ErtugliflozinErtugliflozin (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. |
| 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 |
DapagliflozinDapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4. |
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. |
|
| 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. |
Effects of empagliflozin on AMPK/ACC phosphorylation
|
|
| S8103 |
Sotagliflozin (LX4211)Sotagliflozin (LX4211) is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3. |
||
| 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. |
||
| S0994新 |
Ipragliflozin L-ProlineIpragliflozin 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. |
||
| S8938新 |
KGA-2727KGA-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新 |
MizagliflozinMizagliflozin (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. |
||
| S5566 |
Dapagliflozin propanediol monohydrateDapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors. |
||
| 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 |
PhloretinPhloretin (Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes. |
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 |
PhlorizinPhlorizin (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. |
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 |
ErtugliflozinErtugliflozin (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. |
