A779 |cas:159432-28-7|西域试剂

A779 ,>99%

产品编号：西域试剂-WR371234| CAS NO：159432-28-7| 分子式：C₃₉H₆₀N₁₂O₁₁| 分子量：872.97

A-779是一种G蛋白偶联受体Mas的有效拮抗剂，Mas受体为一种Ang1-7 receptor。A-779抑制Ang-（1-7）的作用，其抑制由Ang II上调的增殖细胞核抗原（PCNA）蛋白表达，但单独的A-779对诱导VSMC的增殖和迁移没有作用。A-779显着升高血清骨特异性碱性磷酸酶（BALP），I型胶原的端肽（CTX），酒石酸盐抗性酸性磷酸酶（TRAcP 5b），骨钙素（OC）和尿脱氧吡啶啉（DPD）。A-779（400 ng/kg/min）对Ang1-7级联的抑制显著消除了卡托普利对骨代谢，矿化和微结构的保护作用。

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货号	包装	价格	库存与货期	购买量	操作
西域试剂-WR371234		￥582.00	杭州北京（现货）
西域试剂-WR371234		￥1350.00	杭州北京（现货）

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产品名称

A779

CAS编号

159432-28-7

产品描述

外观性状

Solid

溶解性

Water 40 mg/mL

溶解性数据

In Vitro:

0.1 M HCL : 25 mg/mL (28.64 mM; ultrasonic and adjust pH to 1 with HCl)

H₂O : 5 mg/mL (5.73 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.1455 mL	5.7276 mL	11.4551 mL
5 mM	0.2291 mL	1.1455 mL	2.2910 mL
10 mM	0.1146 mL	0.5728 mL	1.1455 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

体外研究

A-779 inhibits the effect of Ang-(1-7), which 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. Pretreatment VSMCs with Ang-(1-7) for 5?min significantly inhibits Akt and ERK1/2 phosphorylation induced by Ang II, and this effect is also blocked by A-779, but alone has no effect to induce phosphorylation of Akt and ERK1/2 in VSMCs.

体内研究

Infusion of Ang(1-7) and A-779 (400?ng/kg/min, s.c.) alone or combined for 6 weeks does not prevent uterus atrophy or inhibit the body weight gain of OVX rats. A-779 markedly elevates serum bone specific alkaline phosphatase (BALP), telopeptides of collagen type I (CTX), tartarate resistant acid phosphatase (TRAcP 5b), osteocalcin (OC) and urinary deoxypyridinoline (DPD). Infusion of Ang(1-7) and/or A-779 does not significantly change serum minerals concentrations in sham or OVX groups. A-779 in the OVX animals does not change AngII, Ang(1-7), AT1R, AT2R, ACE, ACE-2, Mas receptor, RANKL and OPG proteins expressions in relation to OVX group, while AngII (P?[1]. Inhibition of Ang1-7 cascade by A-779 (400?ng/kg/min) significantly eradicates captopril protective effects on bone metabolism, mineralization and micro-structure. A-779 also restores OVX effects on RANKL expression and ACE-1/AngII/AT1R cascade and down-regulates OPG expression and ACE-2/Ang1-7/Mas pathway

动物实验