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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