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GKT137831

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Chemical Structure| 1218942-37-0 同义名 : -
CAS号 : 1218942-37-0
货号 : A104916
分子式 : C21H19ClN4O2
纯度 : 97%
分子量 : 394.854
MDL号 : -
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(303.91 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+2% Tween 80+30% PEG 300+water 9 mg/mL

生物活性
描述 Setanaxib (GKT137831) effectively inhibits Nox1/4 (Kis=140±40/110±30 nM)[1]. Setanaxib (GKT137831) administration during a 72-hour normoxia or hypoxia exposure reduces HPASMC proliferation under normoxic conditions at 20 μM but does not affect HPAEC proliferation in normoxia. In prevention studies, Setanaxib (GKT137831) reduces proliferation induced by hypoxia in both HPASMCs and HPAECs at concentrations of 5 and 20 μM. Further tests, including PCNA expression or manual cell counting, confirm that Setanaxib (GKT137831) diminishes hypoxia-induced proliferation in pulmonary vascular cells[2].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03740217 Phase 1 Phase 1 Not yet recruiting April 15, 2019 -
NCT03226067 Primary Biliary Cirrhosis Phase 2 Active, not recruiting September 26, 2019 -
NCT02010242 Type 2 Diabetes Mellitus With ... 展开 >>Diabetic Nephropathy 收起 << Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.66mL

2.53mL

1.27mL

25.33mL

5.07mL

2.53mL
参考文献

[1]Aoyama T, et al. Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent. Hepatology. 2012 Dec;56(6):2316-27.

[2]Green DE, et al. The Nox4 inhibitor GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation. Am J Respir Cell Mol Biol. 2012 Nov;47(5):718-26.