Name: Amiloride HCl
Price: 145.00 USD

- Overview
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    Background
    
    The epithelial sodium channel (ENaC) is a membrane-bound ion-channel that is permeable to protons, Li+-ions, and especially Na+-ions. It is a constitutively active ion-channel. It can be argued that it is the most selective ion channel. In vertebrates, the channels control reabsorption of sodium in kidney, colon, lung and sweat glands. They also play a role in taste perception. Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC).
    In vitro: Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger (NHE) with an IC50 of 3 μM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+]. Amiloride completely inhibits Na+ influx in doses of 1.5 μM in vascular smooth muscle cells [1].
    In vivo: Amiloride at 1 mg/kg/day is found to reverse the initial increases in collagen deposition and prevent further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the stroke-prone spontaneously hypertensive rats. Amiloride antagonizes or prevents actions of aldosterone in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension [1].
    Clinical trial: Amiloride is a potassium-sparing diuretic, first approved for use in 1967, used in the management of hypertension and congestive heart failure. Amiloride was also tested as treatment of cystic fibrosis, but it was revealed inefficient in vivo due to its short time of action.
- Properties
  - Alternative Name
    
    3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide;hydrochloride
    
    CAS Number
    
    2016-88-8
    
    Molecular Formula
    
    C6H8ClN7O·HCl
    
    Molecular Weight
    
    266.09
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥13.3 mg/mL in DMSO; ≥2.48 mg/mL in H2O with ultrasonic; ≥2.57 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Zhou J, Ma S, et al. "Virus-Inspired Mimics: Dual-pH-Responsive Modular Nanoplatforms for Programmable Gene Delivery without DNA Damage with the Assistance of Light." ACS Appl Mater Interfaces. 2020;12(20):22519-22533. PMID:32329598
    2. Wang H, Liu W, et al. "Inhibitor analysis revealed that clathrin-mediated endocytosis is involed in cellular entry of type III grass carp reovirus." Virol J. 2018 May 24;15(1):92. PMID:29793525