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 > Sacubitril
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:
 
Sacubitril
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。
Sacubitril图片
CAS NO:149709-62-6
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
AHU 377
沙库必曲
AHU377
AHU-377
产品介绍
Sacubitril 是一种有效的NEP抑制剂,IC50=5 nM。它是研究心力衰竭药物 LCZ696 的组分之一。

产品描述

AHU-377 is a potent NEP inhibitor with an IC50 of 5 nM. AHU-377 is a component of the heart failure medicine LCZ696.

体外活性

LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and AHU377, a neprilysin inhibitor (1:1 ratio). AHU377 is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657[2]. The inactive NEPi precursor, AHU377, does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy[3].

体内活性

In humans, AHU377 (tmax?0.5-1.1 h) are absorbed quickly. AHU377 is converted rapidly into LBQ657 with its tmax?being reached in 1.9-3.5 h. Mean t1/2?values for the biologically active LBQ657 is 9.9-11.1 h[2].In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 pequivkglmin. This effect is potentiated significantly in animals which receive AHU377. Urinary volume is also potentiated in animals which receive an iv administration of AHU377[1].

Cas No.

149709-62-6

分子式

C24H29NO5

分子量

411.49

别名

AHU 377;沙库必曲;AHU377;AHU-377

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years