3-アミノ-5-[(ヘキサヒドロ-1H-アゼピン)-1-イル]-6-クロロ-N-(アミノイミノメチル)-2-ピラジンカルボアミド 化學(xué)特性,用途語,生産方法
説明
5-(N,N-hexamethylene)-Amiloride (HMA) is a derivative of amiloride with diverse biological activities. It is an allosteric antagonist of adenosine A
2A receptors (K
i = 3.3 μM). 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. It also blocks the cation-selective ion channels formed by the hepatitis C virus (HCV) protein p7. 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. 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.
定義
ChEBI: A member of the class of pyrazines that is amiloride in which the two amino hydrogens at position N-5 are replaced by a hexamethylene moiety, resulting in the formation of an azepane ring.
Biochem/physiol Actions
Inhibitor of Na+/H+ antiport.
3-アミノ-5-[(ヘキサヒドロ-1H-アゼピン)-1-イル]-6-クロロ-N-(アミノイミノメチル)-2-ピラジンカルボアミド 上流と下流の製品情報
原材料
準(zhǔn)備製品