Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Aliskiren hemifumarate (CGP60536B) is an orally active nonpeptide renin inhibitor with antihypertensive activity.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
5 mg | 在庫あり | ¥ 8,000 | |||
10 mg | 在庫あり | ¥ 11,500 | |||
25 mg | 在庫あり | ¥ 13,000 | |||
50 mg | 在庫あり | ¥ 22,500 | |||
100 mg | 在庫あり | ¥ 38,000 | |||
200 mg | 在庫あり | ¥ 68,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 14,500 |
説明 | Aliskiren hemifumarate (CGP60536B) is an orally active nonpeptide renin inhibitor with antihypertensive activity. |
ターゲット&IC50 | Renin:1.5 nM |
In vitro | 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] |
キナーゼ試験 | 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. |
別名 | CGP 60536, SPP 100, CGP60536B |
分子量 | 1219.6 |
分子式 | C30H53N3O6·1/2C4H4O4 |
CAS No. | 173334-58-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (76.3 mM)
H2O: 92 mg/mL (75.4 mM)
Ethanol: 93 mg/mL (76.3 mM)
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Aliskiren hemifumarate 173334-58-2 Autophagy Endocrinology/Hormones RAAS Aliskiren SPP 100 hemifumarate CGP60536B hemifumarate cardiovascular diseases SPP-100 colon carcinoma cachexia cancer CGP 60536 hemifumarate Aliskiren Hemifumarate CGP 60536 Renin inhibit Hypertension C26 SPP 100 SPP100 CGP60536B CGP60536 CGP-60536 Inhibitor inhibitor