Home Metabolism RAAS inhibitor Aliskiren For research use only.

Aliskiren

Synonyms: CGP 60536

Aliskiren(CGP 60536) is a renin inhibitor with antihypertensive activity.

Aliskiren Chemical Structure

Aliskiren Chemical Structure

CAS: 173334-57-1

Selleck's Aliskiren has been cited by 2 publications

Purity & Quality Control

Batch: S576701 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] 6 mg/mL] false Purity: 99.49%
99.49

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Biological Activity

Description Aliskiren(CGP 60536) is a renin inhibitor with antihypertensive activity.
Targets
Renin [1]
In vitro
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 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].
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 551.76 Formula

C30H53N3O6
CAS No. 173334-57-1 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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (181.23 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 6 mg/mL


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In vivo
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