您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > VTP-27999
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
VTP-27999
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。
VTP-27999图片
CAS NO:942142-51-0
规格:98%
分子量:525.08
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议

产品介绍
renin inhibitor, highly potent and selective
CAS:942142-51-0
分子式:C26H41ClN4O5
分子量:525.08
纯度:98%
存储:Store at -20°C

Background:

VTP-27999 is a highly potent and selective renin inhibitor (IC50 = 0.47 nM). It exhibits >1000 selectivity for renin over >150 receptors, ion channels and enzymes.


Renin is an asparyl protease that cleaves angiotensinogen into angiotension I in the plasma. It functions as a regulator of blood pressure and sodium homeostasis.


In vitro, VTP-27999 increases renin immunoreactivity by ≥30%, it bind to acid-activated, intact prorenin and promotes immunoreactivity in a renin assay. In vascular smooth muscle cells, VTP-27999 also blocks renin's ability to activate extracellular signal-regulated kinase 1/2 phosphorylation. [1]


In double transgenic rats engineered to express human renin and angiotensinogen with severe hypertension, 24h treatment of 10 mg/kg VTP-27999 induces a greater reduction in mean arterial blood pressure and a longer duration of action. [2]


参考文献:
1.? Krop M, Lu X, Verdonk K, Schalekamp MA et al. New renin inhibitor VTP-27999 alters renin immunoreactivity and does not unfold prorenin. Hypertension. 2013 May;61(5):1075-82.
2.? Jia L, Simpson RD, Yuan J et al. Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility. ACS Med Chem Lett. 2011 Aug 9;2(10):747-51.