Aliskiren hemifumarate_173334-58-2_DataSheet_MedChemExpress
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Product Name:Aliskiren hemifumarate
CAS No.: 173334-58-2
Product Data Sheet
Cat. No.:HY-12177
MWt:1219.59
Formula:C64H110N6O16
Purity :
>98%
Solubility:
Mechanisms:
Biological Activity: Pathways:Others; Target:Renin
DMSO
gy
Aliskiren hemifumarate is a hemifumarate salt form of Aliskiren. Aliskiren is a direct renin inhibitor
with an IC50 of 0.72?nM against renin. Renin is the first enzyme in the renin-angiotensin-
aldosterone system which plays a role in blood pressure control. Renin cleaves angiotensinogen to
angiotensin I, which is in turn converted by (ACE) to angiotensin II. Angiotensin II has both direct
and indirect effects on blood pressure. It directly causes arterial smooth muscle to contract, leading
to vasoconstriction and increased blood pressure. Angiotensin II also stimulates the production of
aldosterone from the adrenal cortex, which causes the tubules of the kidneys to increase
reabsorption of sodium, with water following thereby increasing plasma volume and blood pressure.
References:
[1]. Ali AK.
Pharmacovigilance analysis of adverse event reports for aliskiren hemifumarate, a first-in-class
direct renin inhibitor.
Ther Clin Risk Manag. 2011;7:337-44.pgygpp
Aliskiren binds to the S3bp binding pocket of renin, essential for its activity. Binding to this pocke...
g
[2]. Kappert K, Unger T, Kintscher U.
Aliskiren hemifumarateDtsch Med Wochenschr. 2008 Jun;133(24):1308-12.
[3]. Ashok S, Varma MS, Swaminathan S.
A Validated LC Method for the Determination of the Enantiomeric Purity of Aliskiren Hemifumarate in
Bulk Drug Samples.
J Chromatogr Sci. 2012 Jun 24.
[4]. Hussar DA.
New drugs: aliskiren hemifumarate, lisdexamfetamine dimesylate, and lapatinib.
JAPhA(2003)2007MJ47(3)425642830
Caution: Not fully tested. For research purposes only
Medchemexpress LLC
www.medchemexpress.comJ Am Pharm Assoc (2003). 2007 May-Jun;47(3):425-6, 428-30.
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