Aliskiren

Catalog No.S5767

For research use only.

Aliskiren is a renin inhibitor with antihypertensive activity.

Aliskiren Chemical Structure

CAS No. 173334-57-1

Selleck's Aliskiren has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description Aliskiren is a renin inhibitor with antihypertensive activity.
Targets
Renin [1]
()
In vitro

Aliskiren is the fourth class of pharmacological agents that modify the function of RAAS. It is an octanamide, is the first known representative of a new class of completely nonpeptide, low-molecular-weight, orally active transition-state renin inhibitors. Aliskiren has good water solubility and low lipophilicity, and is resistant to biodegradation by peptidases in the intestine, blood circulation, and the liver. Aliskiren has 10,000-fold higher affinity for renin than for other aspartic peptidases[1].

In vivo In short-term studies, Aliskiren is effective in lowering blood pressure either alone or in combination with valsartan and hydrochlorothiazide, and had a low incidence of serious adverse effects. Aliskiren has a half-life of approximately 40 h, making it suitable for once-daily dosing, with less potential for loss of efficacy between doses than shorter acting agents. Aliskiren exhibits oral bioavailability due to its low molecular weight (609.8 Da) and nonpeptide structure, making it more resistant to gastrointestinal enzyme disintegration. However, it is still poorly absorbed (oral bioavailability, ∼2.5%). Aliskiren is 50% protein bound, and the apparent volume of distribution is 135 L. Aliskiren is slightly metabolized in humans (about 20%) and is approximately 50% metabolized in rodents. Aliskiren effectively reduces functional plasma renin activity by binding to renin with high affinity, preventing it from converting angiotensinogen to angiotensin I. The inhibition of renin by aliskiren is associated with a reduction in circulating levels of angiotensin I and II, with a resultant increase in plasma renin concentration and inhibit activation of mitogen-activated protein kinases ERK1 (p44) and ERK2 (p42). It prevents hypertrophy and proliferation. Aliskiren is well tolerated, with the most common adverse events reported as headache, dizziness, and fatigue[1].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(181.23 mM)
Ethanol 100 mg/mL
(181.23 mM)
Water 6 mg/mL
(10.87 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 551.76
Formula

C30H53N3O6

CAS No. 173334-57-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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%DMSO %

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Working concentration: mg/ml;

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04432350 Enrolling by invitation -- COVID|Drug Effect|Drug Interaction|Risk Reduction Tabula Rasa HealthCare June 12 2020 --
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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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