product name Aliskiren Hemifumarate
Description: Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM. Aliskiren is the first-in-class drugs called direct renin inhibitors used for the treatment of essential (primary) hypertension. 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.
References: Pharmacol Rep. 2008 Sep-Oct;60(5):623-31; Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705.
609.83
Formula
C30H53N3O6.1/2C4H4O4
CAS No.
173334-58-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (164.0 mM)
Water: 100 mg/mL (164.0 mM)
Ethanol: 100 mg/mL (164.0 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets. Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension. |
| Animal model | |
| Formulation & Dosage | |
| References | Pharmacol Rep. 2008 Sep-Oct;60(5):623-31; Biochem Biophys Res Commun. 2003 Sep 5;308(4):698-705. |
