DPP-4

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研究领域

抑制剂选择性比较

DPP-4产品

所有产品(15) DPP-4抑制剂(15)

目录号	产品描述	文献引用	实验数据
S4002	Sitagliptin phosphate monohydrate Sitagliptin phosphate monohydrate (MK-0431)是一种有效的、选择性的DPP-4口服抑制剂，在Caco-2细胞提取物种IC50为19 nM。	J Biomol Struct Dyn, 2021, 1-12 J Diabetes Res, 2020, 2020:2450781 Circulation, 2017, 135(20):1935-1950	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)是一种高效的，选择性的DPP-4抑制剂，IC50为1 nM。对DPP-4的选择性比对其他二肽基肽酶类如DPP-2、DPP-8和DPP9高10,000倍以上。Linagliptin 在2型糖尿病模型中可激活血小球自噬。DPP4介导TP53缺陷的CRC细胞的铁死亡。	Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 10.1007/s13577-021-00579-z Drug Dev Res, 2021, 10.1002/ddr.21856	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)抑制DPP−4，IC50为2.3 nM。	J Biol Chem, 2020, jbc.RA120.014831 Brain Res Bull, 2019, 147:78-85 Cell Rep, 2017, 20(7):1692-1704
S1540	Saxagliptin (BMS-477118) Saxagliptin (BMS-477118, Onglyza) 是一种选择性的，可逆的DPP4抑制剂，IC50为26 nM。	Turk J Pharm Sci, 2019, 16(2):227-233 Cancer Cell, 2018, 34(4):659-673 J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257	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) benzoate Alogliptin (SYR-322) benzoate是一种有效的，选择性的DPP-4抑制剂，IC50为<10 nM，比作用于DPP-8和DPP-9选择性高10000倍以上。	Cell Rep, 2017, 20(7):1692-1704
E0122^New	Gemigliptin Gemigliptin (Zemiglo, LC15-0444) 是一种有效、选择性和长效的二肽基肽酶 4 (DPP 4) 抑制剂，Ki 为 7.25 nM。相比于各种蛋白酶和肽酶（包括 DPP-8、DPP-9 和成纤维细胞活化蛋白 (FAP)-α），Gemigliptin对 DPP-4 的选择性至少高出 23,000 倍。
S5365	Alogliptin Alogliptin (SYR-322) 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.	Sci Adv, 2021, 7(27)eabh3032
S8565	Omarigliptin (MK-3102) Omarigliptin (MK-3102)是一种竞争性的、可逆的DPP-4抑制剂(IC50 = 1.6 nM, Ki = 0.8 nM)。在所有检测的蛋白酶中，包括QPP, FAP, PEP, DPP8和DPP9等，对DPP-4具有高选择性，具有微弱的离子通道活性（IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5）。	Acta Pharmacol Sin, 2021, 1-9 Front Behav Neurosci, 2021, 15:705579
S5909	Anagliptin Anagliptin是具有口服活性和高选择性的DPP-4抑制剂，IC50为3.3 nM。它通过抑制对NF-κB的激活，发挥对巨噬细胞、脂肪细胞和小鼠肝脏的抗炎活性。
S7513	Trelagliptin Trelagliptin (SYR-472) 是高度选择性的长效的DPP-4抑制剂。
S8455	Talabostat (PT-100) Talabostat (Val-boroPro, PT-100)是二肽基肽酶DPP的抑制剂，对DPP-IV、DPP8、DPP9、QPP、FAP和PEP的IC50值分别为<4 nM、4 nM、11 nM、310 nM、560 nM和390 nM。它具有抗肿瘤和刺激造血作用的活性。	Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.08.015 J Invest Dermatol, 2019, S0022-202X(19)33499-2
S4697	Saxagliptin hydrate Saxagliptin H2O (BMS-477118, Onglyza) 是一种选择性的、可逆的DPP4抑制剂，其IC50为26 nM。	Turk J Pharm Sci, 2019, 16(2):227-233
S4636	Teneligliptin hydrobromide Teneligliptin (Teneligliptin hydrobromide anhydrous)是一种新型的、有效的、长效的dipeptidyl peptidase-4(DPP4)抑制剂。在体外，teneligliptin竞争性地抑制人血浆、大鼠血浆以及人源重组DPP4，IC50约为1 nM。
S5063	Trelagliptin succinate Trelagliptin succinate (SYR472) 是DPP-4抑制剂，被用作新型长效药物，用于2型糖尿病的治疗。
S5079	Sitagliptin Sitagliptin (MK-0431) 是一种具有口服的、具有高度选择性的DPP-4抑制剂，IC50为18 nM。它被用于治疗2型糖尿病。	Med Sci Monit, 2021, 27:e928933 J Biol Chem, 2020, 10.1074/jbc.RA119.010894 J Diabetes Res, 2020, 2020:2450781

目录号	产品描述	文献引用	实验数据
S4002	Sitagliptin phosphate monohydrate Sitagliptin phosphate monohydrate (MK-0431)是一种有效的、选择性的DPP-4口服抑制剂，在Caco-2细胞提取物种IC50为19 nM。	J Biomol Struct Dyn,2021, 1-12 J Diabetes Res,2020, 2020:2450781 Circulation,2017, 135(20):1935-1950	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)是一种高效的，选择性的DPP-4抑制剂，IC50为1 nM。对DPP-4的选择性比对其他二肽基肽酶类如DPP-2、DPP-8和DPP9高10,000倍以上。Linagliptin 在2型糖尿病模型中可激活血小球自噬。DPP4介导TP53缺陷的CRC细胞的铁死亡。	Hum Cell,2021, 10.1007/s13577-021-00639-4 Hum Cell,2021, 10.1007/s13577-021-00579-z Drug Dev Res,2021, 10.1002/ddr.21856	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)抑制DPP−4，IC50为2.3 nM。	J Biol Chem,2020, jbc.RA120.014831 Brain Res Bull,2019, 147:78-85 Cell Rep,2017, 20(7):1692-1704
S1540	Saxagliptin (BMS-477118) Saxagliptin (BMS-477118, Onglyza) 是一种选择性的，可逆的DPP4抑制剂，IC50为26 nM。	Turk J Pharm Sci,2019, 16(2):227-233 Cancer Cell,2018, 34(4):659-673 J Chromatogr B Analyt Technol Biomed Life Sci,2018, 1083:249-257	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) benzoate Alogliptin (SYR-322) benzoate是一种有效的，选择性的DPP-4抑制剂，IC50为<10 nM，比作用于DPP-8和DPP-9选择性高10000倍以上。	Cell Rep,2017, 20(7):1692-1704
E0122^New	Gemigliptin Gemigliptin (Zemiglo, LC15-0444) 是一种有效、选择性和长效的二肽基肽酶 4 (DPP 4) 抑制剂，Ki 为 7.25 nM。相比于各种蛋白酶和肽酶（包括 DPP-8、DPP-9 和成纤维细胞活化蛋白 (FAP)-α），Gemigliptin对 DPP-4 的选择性至少高出 23,000 倍。
S5365	Alogliptin Alogliptin (SYR-322) 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.	Sci Adv,2021, 7(27)eabh3032
S8565	Omarigliptin (MK-3102) Omarigliptin (MK-3102)是一种竞争性的、可逆的DPP-4抑制剂(IC50 = 1.6 nM, Ki = 0.8 nM)。在所有检测的蛋白酶中，包括QPP, FAP, PEP, DPP8和DPP9等，对DPP-4具有高选择性，具有微弱的离子通道活性（IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5）。	Acta Pharmacol Sin,2021, 1-9 Front Behav Neurosci,2021, 15:705579
S5909	Anagliptin Anagliptin是具有口服活性和高选择性的DPP-4抑制剂，IC50为3.3 nM。它通过抑制对NF-κB的激活，发挥对巨噬细胞、脂肪细胞和小鼠肝脏的抗炎活性。
S7513	Trelagliptin Trelagliptin (SYR-472) 是高度选择性的长效的DPP-4抑制剂。
S8455	Talabostat (PT-100) Talabostat (Val-boroPro, PT-100)是二肽基肽酶DPP的抑制剂，对DPP-IV、DPP8、DPP9、QPP、FAP和PEP的IC50值分别为<4 nM、4 nM、11 nM、310 nM、560 nM和390 nM。它具有抗肿瘤和刺激造血作用的活性。	Acta Pharmaceutica Sinica B,2021, 10.1016/j.apsb.2021.08.015 J Invest Dermatol,2019, S0022-202X(19)33499-2
S4697	Saxagliptin hydrate Saxagliptin H2O (BMS-477118, Onglyza) 是一种选择性的、可逆的DPP4抑制剂，其IC50为26 nM。	Turk J Pharm Sci,2019, 16(2):227-233
S4636	Teneligliptin hydrobromide Teneligliptin (Teneligliptin hydrobromide anhydrous)是一种新型的、有效的、长效的dipeptidyl peptidase-4(DPP4)抑制剂。在体外，teneligliptin竞争性地抑制人血浆、大鼠血浆以及人源重组DPP4，IC50约为1 nM。
S5063	Trelagliptin succinate Trelagliptin succinate (SYR472) 是DPP-4抑制剂，被用作新型长效药物，用于2型糖尿病的治疗。
S5079	Sitagliptin Sitagliptin (MK-0431) 是一种具有口服的、具有高度选择性的DPP-4抑制剂，IC50为18 nM。它被用于治疗2型糖尿病。	Med Sci Monit,2021, 27:e928933 J Biol Chem,2020, 10.1074/jbc.RA119.010894 J Diabetes Res,2020, 2020:2450781

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