Home Transmembrane Transporters Sodium Channel inhibitor - Calcium Channel inhibitor - Serine Protease inhibitor Amiloride HCl For research use only.

Amiloride HCl

Synonyms: MK-870 HCl

Amiloride HCl 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).

Amiloride HCl Chemical Structure

Amiloride HCl Chemical Structure

CAS No. 2016-88-8

Purity & Quality Control

Amiloride HCl Related Products

Signaling Pathway

Sodium Channel Signaling Pathways

Sodium Channel Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
D17 Cell viability assay 72 h IC50=110.66 μM 30556178
Abrams Cell viability assay 72 h IC50=121.61 μM 30556178
Dharma Cell viability assay 72 h IC50=148.37 μM 30556178
YD-10B Function assay 4 mM 4 h amiloride strongly blocked the meridianin C‐induced accumulation of vacuoles in YD-10B cells 30246484
NS20Y Function assay Amiloride dose dependently inhibits the ASIC current in NS20Y cells with an IC50 of 11.04 μM 27342076
COS-7 Function assay Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells, Ki=3.28μM 9258366
COS-7 Function assay Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells, Ki=11.6μM 9258366
COS-7 Function assay Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells, Ki=12μM 9258366
MDCK Function assay TP_TRANSPORTER: inhibition of TEA uptake in OCT2-expressing MDCK cells, Ki=4.7μM 11758759
MDCK Function assay TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing MDCK cells, Ki=6.9μM 11758759
AP1 Function assay Inhibition of Amphiuma tridactylum NHE1 mutant containing TM10-12 domain of Pleuronectes americanus expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol, IC50=38μM 17493937
AP1 Function assay Inhibition of Pleuronectes americanus NHE1 C-terminal mutant containing TM7 domain of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol 17493937
AP1 Function assay Inhibition of Pleuronectes americanus NHE1 TM4 mutant containing TFFLF sequence of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol 17493937
HBE Function assay Inhibition of human ENaC in HBE cells by short-circuit current technique, IC50=0.22μM 22197144
FRT Function assay Inhibition of guinea pig ENaCbeta1/gamma1 expressed in FRT cells by short-circuit current technique, IC50=0.54μM 22197144
HBE Function assay Blockade of human ENaC expressed in HBE cells by short-circuit current assay, IC50=0.22μM 22425452
FRT Function assay Blockade of guinea pig ENaC expressed in FRT cells by short-circuit current assay, IC50=0.54μM 22425452
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
AP1 Function assay Inhibition of rat NHE1 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22Na+ influx by liquid scintillation spectroscopy, Ki=1μM ChEMBL
AP1 Function assay Inhibition of full length human C-terminal HA-tagged human NHE5 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22NA+ influx by liquid scintillation spectroscopy, Ki=21μM ChEMBL
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Biological Activity

Description Amiloride HCl 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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT / p-PP1 / PP1 21694768
Immunofluorescence p53 30556178
In Vivo
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]
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 266.09 Formula

C6H8ClN7O.HCl
CAS No. 2016-88-8 SDF --
Smiles C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 53 mg/mL ( (199.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 6 mg/mL

Ethanol : 5 mg/mL


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In vivo
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