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Amiloride HCl

For research use only.

Catalog No.S1811

11 publications

Amiloride HCl  Chemical Structure

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).

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10mM (1mL in DMSO) EUR 127 In stock
EUR 95 In stock
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Selleck's Amiloride HCl has been cited by 11 publications

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Biological Activity

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).
Sodium channel [1] T-type calcium channel [2] uPA [3]
7 μM(Ki)
In vitro

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). [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HBE cells M3;YNGZ2dmO2aX;uJIF{e2G7 MkPNTY5pcWKrdHnvckBw\iCqdX3hckBGVmGFIHnuJGhDTSClZXzsd{BjgSC|aH;yeE1kcXKldXn0JIN2enKnboSgeIVkcG6rcYXlMEBKSzVyPUCuNlIh|ryP MnOzNlIyQTdzNES=
D17 NVvLN5FNS2WubDD2bYFjcWyrdImgZZN{[Xl? NHjiNYM4OiCq NEPacm9KSzVyPUGxNE43PiEQvF2= M{Wzd|MxPTV4MUe4
Abrams Ml7mR4VtdCC4aXHibYxqfHliYYPzZZk> NGH5eok4OiCq MnG1TWM2OD1zMkGuOlEh|ryP NGW2V40{ODV3NkG3PC=>
Dharma MV3D[YxtKH[rYXLpcIl1gSCjc4PhfS=> MVm3NkBp M1TwemlEPTB;MUS4MlM4KM7:TR?= MnTtN|A2PTZzN{i=
YD-10B MkDhSpVv[3Srb36gZZN{[Xl? MlLoOEBuVQ>? M{K5e|QhcA>? Mm\NZY1qdG:{aXTlJJN1em:wZ3z5JIJtd2OtZXSgeIhmKG2ncnnkbYFvcW5iQ,MAlIlv\HWlZXSgZYNkfW23bHH0bY9vKG:oII\hZ5VwdGW|IHnuJHlFNTFyQjDj[Yxtew>? NUjTNGNxOzB{NE[0PFQ>
NS20Y NWjWR5lPTnWwY4Tpc44h[XO|YYm= MWDBcYltd3KrZHWg[I9{\SCmZYDlcoRmdnSueTDpcohq[mm2czD0bIUhSVOLQzDjeZJz\W62IHnuJG5UOjC\IHPlcIx{KHerdHigZY4hUUN3MDDv[kAyOS5yNDFOwG0> MoHTNlc{PDJyN{[=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-AKT / AKT / p-PP1 / PP1 ; 

PubMed: 21694768     

Western blots show significant decreases of cytoplasmic p-Akt, nuclear p-Akt and nuclear p-PP1 in Huh-7 cells treated with amiloride at 0.3 mM and above.


PubMed: 30556178     

Representative images of p53 localization in D17 cells after treatment with high‐dose amiloride (300 μM) or vehicle for 24 hours before p53 staining. Cells were imaged with the Leica DMLB fluorescent microscope. Scale bar 10 μm. 

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. [1]


Solubility (25°C)

In vitro DMSO 53 mg/mL (199.18 mM)
Water 6 mg/mL (22.54 mM)
Ethanol 5 mg/mL (18.79 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 266.09


CAS No. 2016-88-8
Storage powder
in solvent
Synonyms N/A
Smiles C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl

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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 September 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 Recruiting 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID