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。

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

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]

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.

173334-58-2

C30H53N3O6·1/2C4H4O4

1219.6

CGP 60536;CGP60536B;阿利克仑半富马酸盐;SPP 100

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