Name: Amiloride HCl
Brand: Selleck Chemicals
SKU: S1811
Rating: 5 (27 reviews)

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Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.96%

99.96

Verwandte Ziele	CFTR CRM1 CD markers AChR Calcium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Weitere Sodium Channel Inhibitoren	Camostat Mesilate A-803467 cariporide Tolperisone HCl Vinpocetine Veratramine Bulleyaconi cine A GS967 Ambroxol HCl Benzocaine

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Aktivitätsbeschreibung	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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Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht	266.09	Formel	C₆H₈ClN₇O.HCl	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	2016-88-8	--		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	MK-870 HCl			Smiles	C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 53 mg/mL (199.18 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : 6 mg/mL

Ethanol : 5 mg/mL

DMSO : 53 mg/mL (199.18 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : 11 mg/mL

Ethanol : 3 mg/mL

Molaritätsrechner

Masse	Konzentration	Volumen	Molekulargewicht
=	×	×

Verdünnungsrechner Molekulargewichtsrechner

In vivo Charge:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	2.600mg/ml (9.77mM)	Taking the 1 mL working solution as an example, add 50 μL of 52 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	0.440mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH₂O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

Targets/IC₅₀/Ki	Sodium channel T-type calcium channel uPA 7 μM(Ki)
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).
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.
Literatur	[1] https://pubmed.ncbi.nlm.nih.gov/17198922/ [2] https://pubmed.ncbi.nlm.nih.gov/2451291/ [3] https://pubmed.ncbi.nlm.nih.gov/3106085/

Anwendungen (Applications)

Methoden	Biomarker	Bilder	PMID
Western blot	p-AKT / AKT / p-PP1 / PP1		21694768
Immunofluorescence	p53		30556178

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2026-06-11)

NCT-Nummer	Rekrutierung	Erkrankungen	Sponsor/Kooperationspartner	Startdatum	Phasen
NCT06224673	RECRUITING	HER2 Low Breast Carcinoma; Triple Negative Breast Cancer; Hormone-receptor-positive Breast Cancer; Hormone Receptor Positive Breast Carcinoma	Laura Huppert, MD, BA	2026-06-05	PHASE2
NCT05753059	RECRUITING	Heart Failure	Yale University	2023-08-10	PHASE1
NCT04063540	RECRUITING	Migraine With Aura	Centre Hospitalier Universitaire de Nice	2020-08-11	PHASE2
NCT07634068	NOT_YET_RECRUITING	Vertebrobasilar Dolichoectasia	Huashan Hospital	2026-06	PHASE2
NCT06923709	RECRUITING	Chronic Kidney Disease(CKD); Proteinuria	Odense University Hospital	2024-10-10	PHASE2
NCT05228574	COMPLETED	Autosomal Dominant Polycystic Kidney	Erasmus Medical Center	2022-03-11	PHASE4

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Amiloride HCl Sodium Channel Inhibitor

Molekulargewicht: 266.09

Qualitätskontrolle (Quality Control)

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Löslichkeit (Solubility)

Molaritätsrechner

In-vivo-Formulierungsrechner (Klare Lösung)

Wirkmechanismus (Mechanism of Action)

Anwendungen (Applications)

Klinische Studieninformationen (Clinical Trial Information)

Amiloride HCl Sodium Channel Inhibitor

Molekulargewicht: 266.09

Qualitätskontrolle (Quality Control)

Zellkultur, Behandlung & Arbeitskonzentration (Cell Culture, Treatment & Working Concentration)

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Löslichkeit (Solubility)

Molaritätsrechner

In-vivo-Formulierungsrechner (Klare Lösung)

Wirkmechanismus (Mechanism of Action)

Anwendungen (Applications)

Klinische Studieninformationen (Clinical Trial Information)

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)