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 (BI-1356) | <1 mg/mL | 17 mg/mL | '1 mg/mL |
| S3033 | Vildagliptin (LAF-237) | 60 mg/mL | 60 mg/mL | 60 mg/mL |
| S1540 | Saxagliptin (BMS-477118) | 63 mg/mL | 63 mg/mL | '''24 mg/mL |
| S2868 | Alogliptin (SYR-322) benzoate | 2 mg/mL | 68 mg/mL | <1 mg/mL |
| E0122 | Gemigliptin | 12 mg/mL | 98 mg/mL | ''7 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 |
| S5909 | Anagliptin | 20 mg/mL | 77 mg/mL | 77 mg/mL |
| S7513 | Trelagliptin | <1 mg/mL | 71 mg/mL | 3 mg/mL |
| S8455 | Talabostat (PT-100) | 62 mg/mL | 62 mg/mL | 62 mg/mL |
| S4697 | Saxagliptin hydrate | 1 mg/mL | 66 mg/mL | 66 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 (MK-0431) 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 |
Linagliptin (BI-1356)Linagliptin (BI-1356) 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. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells. |
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.
|
|
| S3033 |
Vildagliptin (LAF-237)Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM. |
||
| S1540 |
Saxagliptin (BMS-477118)Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
Mean plasma concentration-time profiles of saxagliptin after oral administration of a test and a reference SPC formulation of saxagliptin/metformin XR tablet (5 mg/500 mg) to 10 healthy Chinese subjects. The inserted represented for the semi-log graph.
|
|
| S2868 |
Alogliptin (SYR-322) benzoateAlogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. |
||
| E0122新 |
GemigliptinGemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α. |
||
| 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). |
||
| S5909 |
AnagliptinAnagliptin is an orally active and highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor and exerts anti-inflammatory effects on macrophages, adipocytes, and mouse livers by suppressing NF-κB activation. |
||
| S7513 |
TrelagliptinTrelagliptin (SYR-472) is a highly selective, long-acting DPP-4 inhibitor. Phase 3. |
||
| S8455 |
Talabostat (PT-100)Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities. |
||
| S4697 |
Saxagliptin hydrateSaxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
||
| S5063 |
Trelagliptin succinateTrelagliptin succinate (SYR472) 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 (MK-0431) 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 (MK-0431) 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 |
Linagliptin (BI-1356)Linagliptin (BI-1356) 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. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells. |
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.
|
|
| S3033 |
Vildagliptin (LAF-237)Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM. |
||
| S1540 |
Saxagliptin (BMS-477118)Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
Mean plasma concentration-time profiles of saxagliptin after oral administration of a test and a reference SPC formulation of saxagliptin/metformin XR tablet (5 mg/500 mg) to 10 healthy Chinese subjects. The inserted represented for the semi-log graph.
|
|
| S2868 |
Alogliptin (SYR-322) benzoateAlogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. |
||
| E0122新 |
GemigliptinGemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α. |
||
| 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). |
||
| S5909 |
AnagliptinAnagliptin is an orally active and highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor and exerts anti-inflammatory effects on macrophages, adipocytes, and mouse livers by suppressing NF-κB activation. |
||
| S7513 |
TrelagliptinTrelagliptin (SYR-472) is a highly selective, long-acting DPP-4 inhibitor. Phase 3. |
||
| S8455 |
Talabostat (PT-100)Talabostat (Val-boroPro, PT-100) is a dipeptidyl peptidase inhibitor with IC50 values of <4 nM, 4 nM, 11 nM, 310 nM, 560 nM and 390 nM for DPP-IV, DPP8, DPP9, QPP, FAP and PEP respectively. It has antineoplastic and hematopoiesis- stimulating activities. |
||
| S4697 |
Saxagliptin hydrateSaxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
||
| S5063 |
Trelagliptin succinateTrelagliptin succinate (SYR472) 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 (MK-0431) 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. |
