DPP-4

信号通路图

研究领域

抑制剂选择性比较

DPP-4产品

所有产品 DPP-4抑制剂(14)

目录号	产品描述	文献引用	实验数据
S4002	Sitagliptin phosphate monohydrate Sitagliptin phosphate monohydrate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。	Circulation, 2017, 135(20):1935-1950 Psychoneuroendocrinology, 2015, 53, 195-206 Sci Rep, 2013, 3:2104	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 Linagliptin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。	J Biol Chem, 2020, 10.1074/jbc.RA119.010894 Cancer Cell Int, 2020, 19;20:58 Free Radic Biol Med, 2018, 114:122-130	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。	Brain Res Bull, 2019, 147:78-85 Cell Rep, 2017, 20(7):1692-1704 FEMS Microbiol Lett, 2016, 363(9)
S1540	Saxagliptin Saxagliptin是一种选择性的，可逆的DPP4抑制剂，IC50为26 nM。	Cancer Cell, 2018, 34(4):659-673 J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257 J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1081-1082:109-117	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
S8455^New	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。	J Invest Dermatol, 2019, S0022-202X(19)33499-2
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.
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）。
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 是高度选择性的长效的DPP-4抑制剂。
S4697	Saxagliptin hydrate Saxagliptin H2O是一种选择性的、可逆的DPP4抑制剂，其IC50为26 nM。
S4636	Teneligliptin hydrobromide Teneligliptin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。	J Biol Chem, 2020, 10.1074/jbc.RA119.010894 Arthritis Rheumatol, 2019, 101002/art41058 Cancer Res, 2018, 78(22):6354-6362

目录号	产品描述	文献引用	实验数据
S4002	Sitagliptin phosphate monohydrate Sitagliptin phosphate monohydrate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。	Circulation,2017, 135(20):1935-1950 Psychoneuroendocrinology,2015, 53, 195-206 Sci Rep,2013, 3:2104	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 Linagliptin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。	J Biol Chem,2020, 10.1074/jbc.RA119.010894 Cancer Cell Int,2020, 19;20:58 Free Radic Biol Med,2018, 114:122-130	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。	Brain Res Bull,2019, 147:78-85 Cell Rep,2017, 20(7):1692-1704 FEMS Microbiol Lett,2016, 363(9)
S1540	Saxagliptin Saxagliptin是一种选择性的，可逆的DPP4抑制剂，IC50为26 nM。	Cancer Cell,2018, 34(4):659-673 J Chromatogr B Analyt Technol Biomed Life Sci,2018, 1083:249-257 J Chromatogr B Analyt Technol Biomed Life Sci,2018, 1081-1082:109-117	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
S8455^New	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。	J Invest Dermatol,2019, S0022-202X(19)33499-2
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.
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）。
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 是高度选择性的长效的DPP-4抑制剂。
S4697	Saxagliptin hydrate Saxagliptin H2O是一种选择性的、可逆的DPP4抑制剂，其IC50为26 nM。
S4636	Teneligliptin hydrobromide Teneligliptin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。	J Biol Chem,2020, 10.1074/jbc.RA119.010894 Arthritis Rheumatol,2019, 101002/art41058 Cancer Res,2018, 78(22):6354-6362

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