A nonpeptide renin inhibitor (IC50 = 0.6 nM) that selectively binds to the S3 sub-pocket of renin

Aliskiren (hemifumarate) – 25 mg

Brand:
Cayman
CAS:
173334-58-2
Storage:
-20
UN-No:
Non-Hazardous - /

Aliskiren is a nonpeptide renin inhibitor (IC50 = 0.6 nM) that selectively binds to the S3 sub-pocket of renin, preventing the conversion of angiotensinogen to angiotensin I, thereby blocking eventual conversion to angiotensin II.{31535,12909} Thus, by blocking renin, aliskiren was designed to prevent angiotensin II-mediated arterial vasoconstriction and aldosterone production.{31535,10615} Aliskiren is orally bioavailable and, in combination with valsartan (Item No. 14178), was shown to reduce blood pressure in db/db mice.{21725}  

 

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Description

A nonpeptide renin inhibitor (IC50 = 0.6 nM) that selectively binds to the S3 sub-pocket of renin, preventing the conversion of angiotensinogen to angiotensin I, thereby blocking eventual conversion to angiotensin II; reduces blood pressure in db/db mice

Formal name: (αS,γS,δS,ζS)-δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-benzeneoctanamide, 2E-butenedioate

Synonyms:  CGP 60536|SPP 100

Molecular weight: 609.8

CAS: 173334-58-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Vasculature|Vasoconstriction||Research Area|Endocrinology & Metabolism|Hormones & Receptors

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