Home Transmembrane Transporters Sodium Channel inhibitor Amiloride HCl dihydrate For research use only.

Amiloride HCl dihydrate

Synonyms: MK-870 hydrochloride dihydrate

Amiloride HCl dihydrate(MK-870 hydrochloride dihydrate) is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.

Amiloride HCl dihydrate Chemical Structure

Amiloride HCl dihydrate Chemical Structure

CAS No. 17440-83-4

Purity & Quality Control

Batch: S256001 DMSO]100 mg/mL]false]Water]5 mg/mL]false]Ethanol]0 mg/mL]false Purity: 100%
100

Amiloride HCl dihydrate Related Products

Signaling Pathway

Sodium Channel Signaling Pathways

Sodium Channel Signaling Pathway

Biological Activity

Description Amiloride HCl dihydrate(MK-870 hydrochloride 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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05044611 Recruiting
Bipolar Disorder
Assistance Publique - Hôpitaux de Paris
 January 11 2023 Phase 4
NCT04181008 Completed
Pharmacokinetics
University of Utah|Center for Addiction and Mental Health
 September 28 2020 Early Phase 1
NCT02323100 Terminated
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

Chemical Information & Solubility

Molecular Weight 302.12 Formula

C6H8ClN7O.HCl.2H2O
CAS No. 17440-83-4 SDF Download Amiloride HCl dihydrate SDF
Smiles C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.O.O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (330.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 5 mg/mL

Ethanol : 0 mg/mL


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In vivo
Batch:

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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.

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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

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