For research use only. Not for use in humans.
Molecular Weight(MW): 609.83
Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM.
Purity & Quality Control
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|Description||Aliskiren hemifumarate is a direct renin inhibitor with IC50 of 1.5 nM.|
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. 
|In vivo||Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets.  Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension. |
-  Nakamura Y, et al. ACS Med Chem Lett, 2012, 3(9), 754–758.
-  Buczko W, et al. Pharmacol Rep, 2008, 60(5), 623-631.
-  Wood JM, et al. Biochem Biophys Res Commun, 2003, 308(4), 698-705.
|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.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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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