Amiloride hydrochloride

Name: Amiloride hydrochloride
Brand: Tocris Bioscience
SKU: 0890
Rating: 4 (2 reviews)

Catalog # 0890 | Tocris Bioscience a Bio-Techne Brand

(2)

Citations (7)

COA / SDS

Na+ channel blocker; also I2 imidazoline ligand

Key Product Details

Description:	Na⁺ channel blocker; also I₂ imidazoline ligand
Chemical Name:	3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	266.09

View Full Technical Details for Amiloride hydrochloride

Technical Data
Citations (7) / Reviews (2)

Biological Activity for Amiloride hydrochloride

Amiloride hydrochloride is a Na⁺ channel blocker. Defines the I_2A-amiloride sensitive and I_2B-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
InChi Key	ACHKKGDWZVCSNH-UHFFFAOYSA-N
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 for Amiloride hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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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References for Amiloride hydrochloride

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

Jetti Evaluation of the role of nitric oxide in acid sensing ion channel mediated cell death. Nitric Oxide 2010 PMID: 20045740
Dai Inhibition of TRPP₃ channel by amil. and analogs. Mol.Pharmacol. 2007 PMID: 17804601
Hamill and McBride The pharmacology of mechanogated membrane ion channels. Pharmacol.Rev. 1996 PMID: 8804105
Ernsberger A second generation of centrally acting antihypertensive agents act on putative I₁-imidazoline receptors. J.Cardiovasc.Pharmacol.
Kleyman Amiloride and its analogues as tools in the study of ion transport. J.Membr.Biol. 1988 PMID: 2852254

Citations for Amiloride hydrochloride (7)

Showing 1 - 7 of 7 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for Amiloride hydrochloride include:

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
Messerschmidt et al. (2019) Osmotic induction of cyclooxygenase-2 in RPE cells: Stimulation of inflammasome activation. Mol Vis. 25:329
PMID: 31341381
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
Barbaro (2017) Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension. Cell Rep. 21(4):1009
PMID: 29069584
Korang-Yeboah et al. (2015) Polycaprolactone/maltodextrin nanocarrier for intracellular drug delivery: formulation, uptake mechanism, internalization kinetics, and subcellular localization. J Neurosci. 10:4763
PMID: 26251597
Jeong et al. (2013) Antinociceptive effects of amil. and benzamil in neuropathic pain model rats. Int J Nanomedicine. 28:1238
PMID: 23960454

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Showing 1 - 7 of 7 citations Showing All

Customer Reviews for Amiloride hydrochloride (2)

4 out of 5

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Drug treatments

Name: Andrew Poon

Species: Other

Assay Type: In Vitro

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.

PMID: 30556178 Reference
ASIC inhibition on acute brain slices

Name: Anonymous

Species: Mouse

Assay Type: In Vivo

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.

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