Aliskiren (CGP 60536)

Description: Aliskiren hemifumarate (CGP 60536), hemifumarate salt form of Aliskiren, is a potent and 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.

Related CAS #: 173334-58-2 (hemifumarate); 173334-57-1(free base)