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Aliskiren(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM. IC50 value: 1.5 nM Target: renin 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. in vivo: Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[3].Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension[4].
| Molecular Weight | 551.76 |
| CAS Number | 173334-57-1 |
| Form | Oil |
| Solubility (25°C) | Ethanol 90 mg/mL DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Saeed Alshahrani. Aliskiren - A promising antioxidant agent beyond hypertension reduction
[3] Kimberly K Daugherty. Aliskiren
| Related Renin Products |
|---|
| Aliskiren Hemifumarate
Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM. |
| Renin substrate 1
Renin substrate 1 is a renin substrate with high affinity to the enzyme. |
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