Amiloride HCl

Catalog No.S1811

Amiloride HCl  Chemical Structure

Molecular Weight(MW): 266.09

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).

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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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).
Targets
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 M4PTPGZ2dmO2aX;uJIF{e2G7 M2HIO2lvcGmkaYTpc44hd2ZiaIXtZY4hTU6jQzDpckBJSkViY3XscJMh[nlic3jvdpQu[2m{Y4XpeEBkfXK{ZX70JJRm[2iwaYH1[UwhUUN3ME2wMlIzKM7:TR?= NX7vTI9YOjJzOUexOFQ>
D17 M4rXR2NmdGxidnnhZoltcXS7IHHzd4F6 NEPPZXM4OiCq M{f5ZWlEPTB;MUGwMlY3KM7:TR?= M3TN[lMxPTV4MUe4
Abrams NXf5c3NIS2WubDD2bYFjcWyrdImgZZN{[Xl? NH7zSJc4OiCq MVLJR|UxRTF{MT62NUDPxE1? NW\mdGQ{OzB3NU[xO|g>
Dharma MUnD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M{W1d|czKGh? NITjVpVKSzVyPUG0PE4{PyEQvF2= NUXpbVdYOzB3NU[xO|g>
YD-10B NUjEcpFJTnWwY4Tpc44h[XO|YYm= M37zO|QhdU1? MX60JIg> NHPVSm5idWmub4Lp[IUhe3S{b37ncJkh[myxY3vl[EB1cGVibXXybYRq[W6rbjDD5qCRcW6mdXPl[EBi[2O3bYXsZZRqd25ib3[geoFkfW:uZYOgbY4hYURvMUDCJINmdGy| M4DGV|MxOjR4NEi0
NS20Y MX7GeY5kfGmxbjDhd5NigQ>? M1:5RmFucWyxcnnk[UBld3OnIHTldIVv\GWwdHz5JIlvcGmkaYTzJJRp\SCDU1nDJIN2enKnboSgbY4hVlN{MGmgZ4VtdHNid3n0bEBidiCLQ{WwJI9nKDFzLkC0JO69VQ>? NH\zTGMzPzN2MkC3Oi=>

... Click to View More Cell Line Experimental Data

Assay
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.

21694768
Immunofluorescence
p53; 

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. 

30556178
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]

Protocol

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
Formula

C6H8ClN7O.HCl

CAS No. 2016-88-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02323100 Recruiting 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
NCT01918488 Unknown status Dietary Supplement: Standardized salt diet|Drug: Amiloride Diabetic Nephropathies|Hypertension University of Southern Denmark|Odense University Hospital|Region of Southern Denmark|The Ministry of Science Technology and Innovation Denmark|Danish Heart Foundation October 2013 Not Applicable

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Sodium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID