For research use only.
CAS No. 2016-88-8
Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
Selleck's Amiloride HCl has been cited by 6 publications
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|Description||Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).|
Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC50 (the concentration required to reach 50% inhibition of an ion channel) in the concentration range of 0.1 to 0.5 μM. Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger (NHE) with an IC50 as low as 3 μM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+]. Amiloride is an even weaker inhibitor of the Na+/Ca2+ exchanger (NCX), with an IC50 of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na+ influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC). 
|In vivo||Amiloride at 1 mg/kg/day subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP). compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension. |
|In vitro||DMSO||53 mg/mL (199.18 mM)|
|Water||6 mg/mL (22.54 mM)|
|Ethanol||5 mg/mL (18.79 mM)|
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In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04181008||Recruiting||Drug: Amiloride||Pharmacokinetics||University of Utah|Center for Addiction and Mental Health||July 28 2020||Early Phase 1|
|NCT02323100||Suspended||Drug: Ravicti low dose|Drug: Ravicti high dose|Drug: Placebo||Cystic Fibrosis||National Jewish Health|University of Alabama at Birmingham|Children''s Hospital of Philadelphia|Johns Hopkins University|Horizon Pharma Ireland Ltd. Dublin Ireland||December 2 2018||Phase 1|Phase 2|
|NCT02586883||Unknown status||Other: bronchial ddp test||Idiopathic Dilation of the Bronchi||Assistance Publique - Hôpitaux de Paris||March 29 2016||Not Applicable|
|NCT02325362||Completed||Drug: Miglustat ; placebo|Drug: Placebo ; Miglustat||Cystic Fibrosis||Assistance Publique - Hôpitaux de Paris|Actelion|CRCM (Centres de Ressources et de Compétences de la Mucoviscidose)||March 17 2015||Phase 2|Phase 3|
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