DPP-4
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 | ||
| S4002 | Sitagliptin phosphate monohydrate | 41 mg/mL | 100 mg/mL | <1 mg/mL |
| S3031 | Linagliptin | <1 mg/mL | 17 mg/mL | 1 mg/mL |
| S5365 | Alogliptin | 18 mg/mL | 67 mg/mL | 67 mg/mL |
| S8565 | Omarigliptin (MK-3102) | <1 mg/mL | 79 mg/mL | <1 mg/mL |
| S5063 | Trelagliptin succinate | 95 mg/mL | 95 mg/mL | 5 mg/mL |
| S5079 | Sitagliptin | -1 mg/mL | 81 mg/mL | -1 mg/mL |
DPP-4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 |
|---|---|---|---|
| S4002 |
Sitagliptin phosphate monohydrateSitagliptin phosphate monohydrate is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts. |
Functional lack of DPP4 activity was confirmed in plasma samples from DPP4mut rats, as compared to DAwt (E, white and dark bars) and to rats treated with sitagliptin for three weeks (E, light gray bars). Specificity of the assay was further confirmed by inhibition of the measured peptidase activity with sitagliptin, in vitro. |
|
| S3031 |
LinagliptinLinagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. |
Effect of linagliptin on oxidative stress in rat hearts suffered from 9 h of hypothermic preservation followed by 60 min of reperfusion. (A) Representative image of NOX2 detected by western blotting. (B). Densitometric analysis showing the expression of NOX2 using β‑actin for normalization. Data are mean ± S.E.M. (n = 3) and expressed as fold increase relative to the value of control group. (C-E) Measurement of MnSOD activity, ROS and MDA content. Data are expressed as mean ± S.E.M., n = 8. *P < 0.05, **P < 0.01 vs control group; #P < 0.05, ##P < 0.01 vs Celsior group. NOX2: NADPH oxidase 2; MnSOD: manganese superoxide dismutase; ROS: reactive oxygen species; MDA: malondialdehyde.
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| S5365 |
AlogliptinAlogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4)with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. |
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| S8565 |
Omarigliptin (MK-3102)Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5). |
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| S5063 |
Trelagliptin succinateTrelagliptin succinate is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM). |
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| S5079 |
SitagliptinSitagliptin is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes. |
| 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 |
|---|---|---|---|
| S4002 |
Sitagliptin phosphate monohydrateSitagliptin phosphate monohydrate is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts. |
Functional lack of DPP4 activity was confirmed in plasma samples from DPP4mut rats, as compared to DAwt (E, white and dark bars) and to rats treated with sitagliptin for three weeks (E, light gray bars). Specificity of the assay was further confirmed by inhibition of the measured peptidase activity with sitagliptin, in vitro. |
|
| S3031 |
LinagliptinLinagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. |
Effect of linagliptin on oxidative stress in rat hearts suffered from 9 h of hypothermic preservation followed by 60 min of reperfusion. (A) Representative image of NOX2 detected by western blotting. (B). Densitometric analysis showing the expression of NOX2 using β‑actin for normalization. Data are mean ± S.E.M. (n = 3) and expressed as fold increase relative to the value of control group. (C-E) Measurement of MnSOD activity, ROS and MDA content. Data are expressed as mean ± S.E.M., n = 8. *P < 0.05, **P < 0.01 vs control group; #P < 0.05, ##P < 0.01 vs Celsior group. NOX2: NADPH oxidase 2; MnSOD: manganese superoxide dismutase; ROS: reactive oxygen species; MDA: malondialdehyde.
|
|
| S5365 |
AlogliptinAlogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4)with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. |
||
| S8565 |
Omarigliptin (MK-3102)Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5). |
||
| S5063 |
Trelagliptin succinateTrelagliptin succinate is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM). |
||
| S5079 |
SitagliptinSitagliptin is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes. |
