Aliskiren hemifumarate
作者：齐岳
发布时间：2023-09-13
17:32:04
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产品名称：Aliskiren hemifumarate
产品描述：
| 产品描述 | Aliskiren Hemifumarate is an orally active nonpeptide renin inhibitor with antihypertensive activity. |
| 靶点活性 | Renin:1.5 nM |
| 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. |
| 别名 | 阿利克仑半富马酸盐, CGP 60536, CGP60536B, SPP 100 |
| 分子量 | 1219.6 |
| 分子式 | C30H53N3O6·1/2C4H4O4 |
| CAS No. | 173334-58-2 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 93 mg/mL (76.3 mM)
H2O: 92 mg/mL (75.4 mM)
Ethanol: 93 mg/mL (76.3 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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