An amiloride derivative with diverse biological activities; an allosteric antagonist of adenosine A2A receptors (Ki = 3.3 µM); inhibits the cation-selective ion channel formed by Vpu at 50 µM

5-(N,N-hexamethylene)-Amiloride – 25 mg

Brand:
Cayman
CAS:
1428-95-1
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

5-(N,N-hexamethylene)-Amiloride (HMA) is a derivative of amiloride (Item No. 14409) with diverse biological activities.{53366,53368,53367,53369,53370} It is an allosteric antagonist of adenosine A2A receptors (Ki = 3.3 µM).{53368} HMA inhibits the cation-selective ion channel formed by the HIV-1 viral protein Vpu when used at a concentration of 50 µM, as well as budding of virus-like particles in HeLa cells expressing the HIV-1 proteins Gag and Vpu when used at a concentration of 10 µM.{53366} It also blocks the cation-selective ion channels formed by the hepatitis C virus (HCV) protein p7.{53367} HMA (40 µM) induces necrosis in and reduces the viability of MCF-7, MDA-MB-231, T47D, SK-BR-3, Met-1, and NDL breast cancer cells but not cardiomyocytes or uterine, pulmonary, and renal epithelial cells.{53369} HMA protects against post-ischemic contractile dysfunction and reduces coronary effluent creatine phosphokinase activity in a model of ischemia-reperfusion injury using isolated rat right ventricular free walls.{53370}  

 

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Description

An amiloride derivative with diverse biological activities; an allosteric antagonist of adenosine A2A receptors (Ki = 3.3 µM); inhibits the cation-selective ion channel formed by Vpu at 50 µM, as well as budding of virus-like particles in HeLa cells expressing the HIV-1 proteins Gag and Vpu at 10 µM; blocks the cation-selective ion channels formed by p7; induces necrosis in and reduces the viability of various breast cancer cells at 40 µM; protects against post-ischemic contractile dysfunction and reduces coronary effluent creatine phosphokinase activity in a model of ischemia-reperfusion injury using isolated rat right ventricular free walls

Formal name: 3-amino-N-(aminoiminomethyl)-6-chloro-5-(hexahydro-1H-azepin-1-yl)-2-pyrazinecarboxamide

Synonyms:  HMA

Molecular weight: 311.8

CAS: 1428-95-1

Purity: ≥98%

Formulation: A crystalline solid

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