Amiloride HCl dihydrate

Catalog No.S2560

For research use only.

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

Amiloride HCl dihydrate Chemical Structure

CAS No. 17440-83-4

Selleck's Amiloride HCl dihydrate has been cited by 8 Publications

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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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 302.12
Formula

C6H8ClN7O.HCl.2H2O

CAS No. 17440-83-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.O.O.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05044611 Not yet recruiting Drug: Anhydrous Amiloride Hydrochloride|Drug: Placebo Bipolar Disorder Assistance Publique - Hôpitaux de Paris April 1 2022 Phase 4
NCT04181008 Recruiting Drug: Amiloride Pharmacokinetics University of Utah|Center for Addiction and Mental Health September 28 2020 Early Phase 1
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 Completed Other: bronchial ddp test Idiopathic Dilation of the Bronchi Assistance Publique - Hôpitaux de Paris March 29 2016 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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