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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 34.00 | |
10 mg | In stock | $ 50.00 | |
25 mg | In stock | $ 55.00 | |
50 mg | In stock | $ 98.00 | |
100 mg | In stock | $ 164.00 | |
200 mg | In stock | $ 297.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 62.00 |
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. |
Synonyms | CGP 60536, SPP 100, CGP60536B |
Molecular Weight | 1219.6 |
Formula | 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. More
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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