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Aliskiren hemifumarate (CGP60536B) is an orally active nonpeptide renin inhibitor with antihypertensive activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $34 | In Stock | |
10 mg | $50 | In Stock | |
25 mg | $55 | In Stock | |
50 mg | $98 | In Stock | |
100 mg | $164 | In Stock | |
200 mg | $297 | In Stock | |
1 mL x 10 mM (in DMSO) | $62 | In Stock |
Description | Aliskiren hemifumarate (CGP60536B) is an orally active nonpeptide renin inhibitor with antihypertensive activity. |
Targets&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] |
Kinase Assay | 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. |
Alias | SPP 100, CGP60536B, CGP 60536 |
Molecular Weight | 1219.6 |
Formula | C30H53N3O6·1/2C4H4O4 |
Cas No. | 173334-58-2 |
Smiles | C(=O)(/C=C/C(=O)O)O.C(=O)([C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)Cc1cc(c(cc1)OC)OCCCOC)N)O)C(C)C)NCC(C(=O)N)(C)C.C(=O)([C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)Cc1cc(c(cc1)OC)OCCCOC)N)O)C(C)C)NCC(C(=O)N)(C)C |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 93 mg/mL (76.3 mM) H2O: 92 mg/mL (75.4 mM) Ethanol: 93 mg/mL (76.3 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
H2O/DMSO/Ethanol
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