购物车
- 全部删除
- 您的购物车当前为空
A 779 是一种 G 蛋白偶联受体 Mas 的有效拮抗剂,Mas 受体是Ang1-7 receptor,与传统的AngII 不同。
A 779 是一种 G 蛋白偶联受体 Mas 的有效拮抗剂,Mas 受体是Ang1-7 receptor,与传统的AngII 不同。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 1,870 | 35日内发货 |
产品描述 | A 779 is a potent antagonist of the G-protein-coupled receptor Mas, the Ang1-7 receptor, which is distinct from conventional AngII. |
体外活性 | A 779抑制了由Ang II上调的增殖细胞核抗原(PCNA)蛋白表达,但A 779单独使用并不诱导VSMCs的增殖和迁移。预处理Ang-(1-7)显著延缓了Ang II诱导的VSMCs炎症反应,这一反应与MCP-1、VCAM-1和IL-1β的表达上调有关,而Ang-(1-7)的这种效果被A 779阻断。但A 779单独使用并不诱发VSMCs的炎症反应[1]。 |
体内活性 | A 779通过抑制Ang1-7级联反应,显著消除了卡托普利对骨代谢、矿化和微观结构保护作用。此外,A 779还恢复了卵巢切除(OVX)对RANKL表达的影响,以及对ACE-1/AngII/AT1R级联反应的影响,下调了OPG表达和ACE-2/Ang1-7/Mas途径。与临床观察到的继ACE-1抑制后骨保护特性一致,ACE-2/Ang1-7/Mas信号的局部激活和骨吸收的抑制似乎是卡托普利骨保护效应的责任机制,这可能为治疗残疾性骨骼和骨骼肌疾病提供潜在的治疗价值。 |
细胞实验 | HUVECs were cultured in vitro and divided into six groups:?the control group (normal medium), the ox-LDL group(treated with 75 mg/L ox-LDL), the ox-LDL+ Ang-(1-7) group (1 μmol/L Ang-(1-7) pretreated for 30 minutes, then intervened with 75 mg/L ox-LDL), the ox-LDL+ Ang-(1-7)+ A-779 group(1 μmol/L A-779 (Mas receptor) pretreated for 30 minutes, 1 μmol/L Ang-(1-7) pretreated for 30 minutes, then intervened with 75 mg/L ox-LDL), the ox-LDL+ A-779 group (1 μmol/L A-779 pretreated for 30 minutes, then intervened with 75 mg/L ox-LDL),?the ox-LDL+ HTA125 group (10 μg/L HTA125 (TLR4-blocking antibody) pretreated for 30 minutes, then intervened with 75 mg/L ox-LDL ).?The corresponding index was detected after 24 hours after intervention.?Apoptosis of cells were detected by Annexin V-FITC/PI double staining flow cytometry and transferase-mediated deoxyuridine triphosphate-biotin nick end labeling (TUNEL).?The generation of reactive oxygen species (ROS), products in oxidative stress, were detected by DCFH-DA staining.?The mRNA and protein expression levels of NADPH oxidase 4(NOX4) and TLR4 were detected by real-time reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting analysis respectively[1]. |
分子量 | 872.97 |
分子式 | C39H60N12O11 |
CAS No. | 159432-28-7 |
Smiles | [H][C@](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](N)CC(O)=O)C(C)C)([C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C)C(O)=O |
密度 | 1.45 g/cm3 (Predicted) |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | H2O: 50 mg/mL (57.28 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容