Home Endocrinology & Hormones RAAS inhibitor Aliskiren Hemifumarate For research use only.

Aliskiren Hemifumarate

Synonyms: CGP 60536 hemifumarate, CGP60536B hemifumarate, SPP 100 hemifumarate

Aliskiren hemifumarate(CGP 60536 hemifumarate, CGP60536B hemifumarate, SPP 100 hemifumarate) is a direct renin inhibitor with IC50 of 1.5 nM.

Aliskiren Hemifumarate Chemical Structure

Aliskiren Hemifumarate Chemical Structure

CAS: 173334-58-2

Selleck's Aliskiren Hemifumarate has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Biological Activity

Description Aliskiren hemifumarate(CGP 60536 hemifumarate, CGP60536B hemifumarate, SPP 100 hemifumarate) is a direct renin inhibitor with IC50 of 1.5 nM.
Targets
Renin [1]
1.5 nM
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04432350 Withdrawn COVID|Drug Effect|Drug Interaction|Risk Reduction Tabula Rasa HealthCare June 12 2020 --
NCT01570686 Completed Hypertension Novartis Pharmaceuticals|Novartis April 2012 Phase 4
NCT01519635 Completed Hypertension Centre Hospitalier Universitaire Vaudois October 2011 Phase 4
NCT01235910 Terminated Hypertension|Cardiac Transplantation University of Colorado Denver|American Heart Association May 2011 Phase 4
NCT01237873 Completed Essential Hypertension Novartis Pharmaceuticals|Novartis January 2011 Phase 3

Chemical lnformation & Solubility

Molecular Weight 609.83 Formula

C30H53N3O6.1/2C4H4O4
CAS No. 173334-58-2 SDF Download Aliskiren Hemifumarate SDF
Smiles CC(C)C(CC1=CC(=C(C=C1)OC)OCCCOC)CC(C(CC(C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.CC(C)C(CC1=CC(=C(C=C1)OC)OCCCOC)CC(C(CC(C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 122 mg/mL ( (200.05 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 122 mg/mL

Ethanol : 122 mg/mL


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In vivo
Batch:

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

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