Amiloride hydrochloride

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Description: Na+ channel blocker; also I2 imidazoline ligand
Chemical Name: 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride
Purity: ≥98% (HPLC)
Citations (7)
Reviews (2)

Biological Activity for Amiloride hydrochloride

Amiloride hydrochloride is a Na+ channel blocker. Defines the I2A-amiloride sensitive and I2B-amiloride insensitive imidazoline binding Blocks TRPP3, acid sensing- (ASIC) and mechanogated membrane-ion channels, as well as the Na+/H+ exchanger. Also inhibits urokinase-type plasminogen activator (uPA); has no effect on tissue-type plasminogen activator.

Technical Data for Amiloride hydrochloride

M. Wt 266.09
Formula C6H8ClN7O.HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 2016-88-8
PubChem ID 16230
Smiles Cl.NC(=N)NC(=O)C1=NC(Cl)=C(N)N=C1N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Amiloride hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 1.33 5 with gentle warming
DMSO 26.61 100

Preparing Stock Solutions for Amiloride hydrochloride

The following data is based on the product molecular weight 266.09. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.76 mL 18.79 mL 37.58 mL
5 mM 0.75 mL 3.76 mL 7.52 mL
10 mM 0.38 mL 1.88 mL 3.76 mL
50 mM 0.08 mL 0.38 mL 0.75 mL

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Product Datasheets for Amiloride hydrochloride

Certificate of Analysis / Product Datasheet
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References for Amiloride hydrochloride

References are publications that support the biological activity of the product.

Dai et al (2007) Inhibition of TRPP3 channel by amil. and analogs. Mol.Pharmacol. 72 1576 PMID: 17804601

Hamill and McBride (1996) The pharmacology of mechanogated membrane ion channels. Pharmacol.Rev. 48 231 PMID: 8804105

Kleyman et al (1988) Amiloride and its analogues as tools in the study of ion transport. J.Membr.Biol. 105 1 PMID: 2852254

Ernsberger et al (1992) A second generation of centrally acting antihypertensive agents act on putative I1-imidazoline receptors. J.Cardiovasc.Pharmacol. 20 S1

Jetti et al (2010) Evaluation of the role of nitric oxide in acid sensing ion channel mediated cell death. Nitric Oxide 22 213 PMID: 20045740

Vassalli et al (1987) Amiloride selectively inhibits the urokinase-type plasminogen activator. 214 187 PMID: 3106085

If you know of a relevant reference for Amiloride hydrochloride, please let us know.

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7 Citations for Amiloride hydrochloride

Citations are publications that use Tocris products. Selected citations for Amiloride hydrochloride include:

Poon et al (2018) Effects of the potassium-sparing diuretic amil. on chemotherapy response in canine osteosarcoma cells. J Vet Intern Med 33 800 PMID: 30556178

Jeong et al (2013) Antinociceptive effects of amil. and benzamil in neuropathic pain model rats. Int J Nanomedicine 28 1238 PMID: 23960454

Neubert et al (2020) NCX1 Represents an Ionic Na+ Sensing Mechanism in Macrophages PloS Biol 18 PMID: 32569301

Roebber et al (2019) The Role of the Anion in Salt (NaCl) Detection by Mouse Taste Buds. J Neurosci 39 6224 PMID: 31171579

Do you know of a great paper that uses Amiloride hydrochloride from Tocris? Please let us know.

Reviews for Amiloride hydrochloride

Average Rating: 4 (Based on 2 Reviews.)

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Drug treatments.
By Andrew Poon on 03/01/2019
Assay Type: In Vitro
Species: Other

Amiloride was combined with chemotherapy to assess its potential to kill canine osteosarcoma cells, and was found to be synergistic with doxorubicin chemotherapy. It was also used by the Seahorse analyzer to show that the extracellular acidification rate (ECAR) decreases after amiloride exposure.

Dissolve the powder in 100 mM DMSO, and dilute according to minimize vehicle effects.

review image

ASIC inhibition on acute brain slices.
By Anonymous on 01/10/2018
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: acute brain slice

Used to show ASIC channels were not involved in the studied effect. No effect was had, as expected, however it's hard to control for the drug efficacy as we did not show ASIC blockade directly.