Aliskiren Hemifumarate

Catalog No.S2199

Aliskiren Hemifumarate Chemical Structure

Molecular Weight(MW): 609.83

Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM.

Size Price Stock Quantity  
In DMSO USD 100 In stock
USD 97 In stock
USD 157 In stock
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Biological Activity

Description Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM.
Targets
Renin [1]
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]

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]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (163.98 mM)
Water 100 mg/mL (163.98 mM)
Ethanol 100 mg/mL (163.98 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 609.83
Formula

C30H53N3O6.1/2C4H4O4

CAS No. 173334-58-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01570686 Completed Drug: Aliskiren Hypertension Novartis Pharmaceuticals|Novartis April 2012 Phase 4
NCT01519635 Completed Drug: Aliskiren|Drug: Hydrochlorothiazide Hypertension Centre Hospitalier Universitaire Vaudois October 2011 Phase 4
NCT01235910 Terminated Drug: Aliskiren Hypertension|Cardiac Transplantation University of Colorado Denver|American Heart Association May 2011 Phase 4
NCT01237873 Completed Drug: Ali/Amlo 150/2.5 mg Essential Hypertension Novartis Pharmaceuticals|Novartis January 2011 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID