Amiloride HCl dihydrate

Catalog No.S2560

Amiloride HCl dihydrate Chemical Structure

Molecular Weight(MW): 302.12

Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.

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Biological Activity

Description Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.
Targets
Sodium channel [1]
In vitro

Amiloride also induces the dephosphorylation of P13K (phosphatidylinositol 3-kinase) and PDK-1 (phosphoinositide-dependent kinase-1) kinases along with PTEN (phosphatase and tensin homolog deleted on chromosome 10) and PP1 alpha phosphatases. Amiloride inhibits phosphorylation of kinases and phosphatases by competing with ATP. Amiloride, which causes little or no cytotoxicity by itself, enhances TRAIL-induced apoptosis. [1] Amiloride precludes the alkalinization and in parallel inhibit cellular proliferation. Amiloride directly inhibits autophosphorylation of the EGF receptor. [2] Amiloride significantly enhances recovery to a maximum of 39%, 88%, and 78% for force, +dF/dt, and -dF/dt, respectively. [3] Amiloride, a frequently used inhibitor of Na+/H+ exchange, rapidly inhibits phorbol ester-stimulated protein phosphorylation in vivo and protein kinase C-mediated phosphorylation in vitro, both with potency similar to that with which Amiloride inhibits Na+/H+ exchange. Amiloride blocks phorbol ester-induced adhesion of HL-60 cells (adhesion being a property indicative of the differentiated state), but dimethylamiloride (as well as ethylisopropylamiloride, another very potent amiloride analog) does not. [4] Amiloride inhibits the ouabain-sensitive rate of oxygen consumption (QO2) of a suspension of rabbit intact proximal tubules in the presence of different concentrations of extracellular sodium. [5]

Protocol

Solubility (25°C)

In vitro Water 17 mg/mL (56.26 mM)
DMSO 0 mg/mL (0.0 mM)
Ethanol 0 mg/mL (0.0 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 302.12
Formula

C6H8ClN7O.HCl.2H2O

CAS No. 17440-83-4
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