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

Purity & Quality Control

Choose Selective Sodium Channel Inhibitors

Other Sodium Channel Products

Biological Activity

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


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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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, 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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Amiloride HCl dihydrate | Amiloride HCl dihydrate ic50 | Amiloride HCl dihydrate price | Amiloride HCl dihydrate cost | Amiloride HCl dihydrate solubility dmso | Amiloride HCl dihydrate purchase | Amiloride HCl dihydrate manufacturer | Amiloride HCl dihydrate research buy | Amiloride HCl dihydrate order | Amiloride HCl dihydrate mouse | Amiloride HCl dihydrate chemical structure | Amiloride HCl dihydrate mw | Amiloride HCl dihydrate molecular weight | Amiloride HCl dihydrate datasheet | Amiloride HCl dihydrate supplier | Amiloride HCl dihydrate in vitro | Amiloride HCl dihydrate cell line | Amiloride HCl dihydrate concentration | Amiloride HCl dihydrate nmr