keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 suppresses the proliferating cell nuclear antigen (PCNA) protein expression up-regulated by Ang II, but A-779 alone has no effect to induce proliferation and migration of VSMCs.?Pretreatment with Ang-(1-7) significantly retards Ang II-induced inflammatory responses of VSMCs associated with up-regulated MCP-1, VCAM-1 and IL-1β expressions, and this effect of Ang-(1-7) is blocked by A-779.?But A-779 alone has no effect to induce inflammatory response of VSMCs[1]. |
体内活性 | Inhibition of Ang1-7 cascade by A-779 significantly eradicated captopril protective effects on bone metabolism, mineralization and micro-structure.?A-779 also restored OVX effects on RANKL expression and ACE-1/AngII/AT1R cascade and down-regulated OPG expression and ACE-2/Ang1-7/Mas pathway.?In line with the clinical observations of the bone-preservative properties following ACE-1 inhibition, local activation of ACE-2/Ang1-7/Mas signaling and suppressed osteoclastogenesis seem responsible for the osteo-preservative effect of captopril, which could offers a potential therapeutic value in treatment of disabling bone and skeletal muscular diseases[2]. |
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 |
keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 50 mg/mL (57.28 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 1.1455 mL | 5.7276 mL | 11.4551 mL | 28.6379 mL |
5 mM | 0.2291 mL | 1.1455 mL | 2.291 mL | 5.7276 mL | |
10 mM | 0.1146 mL | 0.5728 mL | 1.1455 mL | 2.8638 mL | |
20 mM | 0.0573 mL | 0.2864 mL | 0.5728 mL | 1.4319 mL | |
50 mM | 0.0229 mL | 0.1146 mL | 0.2291 mL | 0.5728 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
A 779 159432-28-7 Endocrinology/Hormones RAAS Inhibitor inhibit A-779 Angiotensin Receptor A779 inhibitor