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Aliskiren Hemifumarate
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。
CAS NO:173334-58-2
包装与价格:
包装价格(元)
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
CGP 60536
CGP60536B
阿利克仑半富马酸盐
SPP 100
产品介绍
Aliskiren hemifumarate 一种可口服非肽肾素抑制剂,IC50为1.5 nM,具有抗高血压活性。

产品描述

Aliskiren Hemifumarate is an orally active nonpeptide renin inhibitor with antihypertensive activity.

体外活性

Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans. [2]

激酶实验

Radioligand Binding Assay: Human CB1 and CB2 stably transfect HEK 293 cells and cell membrane is purified. 0.2-8 μg of the purified membrane is incubated with 0.75 nM [3H] CP55,940 and Rimonabant in the incubation buffer (50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, 0.3%BSA, pH 7.4). The non-specific binding is defined in the presence of 1 μM of CP55,940. The reactions are incubated for one and a half hours at 30 °C in Multiscreen. The reactions are terminated by manifold filtration and washed four times with ice-cold wash buffer (50 mM Tris, pH 7.4, 0.25% BSA).The radioactivity bound to the filters is measured by Topcount. The IC50 is determined as the concentration of Rimonabant required to inhibit 50% of the binding of [3H] CP55,940 and calculated by non-linear regression.

Cas No.

173334-58-2

分子式

C30H53N3O6·1/2C4H4O4

分子量

1219.6

别名

CGP 60536;CGP60536B;阿利克仑半富马酸盐;SPP 100

储存和溶解度

Ethanol:93 mg/mL (76.3 mM)
H2O:92 mg/mL (75.4 mM)
DMSO:93 mg/mL (76.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years