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A 779
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
A 779图片
CAS NO:159432-28-7
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品名称
A 779(3TFA)
产品介绍
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(3TFA) is a potent antagonist of angiotensin-(1-7) receptor

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].

Cas No.

159432-28-7

分子式

C39H60N12O11

分子量

872.982

别名

A 779(3TFA)

储存和溶解度

H2O:50 mg/mL (57.28 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years