Amiloride hydrochloride

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Cat.No. 0890 - Amiloride hydrochloride | C6H8ClN7O.HCl | CAS No. 2016-88-8
Description: Na+ channel blocker; also I2 imidazoline ligand
Chemical Name: 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride
Purity: ≥98% (HPLC)
Citations (3)

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 26.61 100
water 2.66 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 266.09. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet


References are publications that support the products' biological activity.

Dai et al (2007) Inhibition of TRPP3 channel by amiloride 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 PMID:

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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Keywords: Amiloride hydrochloride, supplier, I2, selective, ligands, differentiates, I2A, I2B, Na+, channel, blockers, Imidazoline, Receptors, Sodium, NaV, Channels, voltage-gated, voltage-dependent, NHE, Na+, H+, exchanger, ASIC, upa, urokinase-type, plasminogen, inhibitors, inhibits, I2, Receptors, Voltage-gated, Sodium, Channels, Na+/H+, Exchanger, TRPP, ASIC, Urokinase, Voltage-gated, Sodium, Channels, Tocris Bioscience

3 Citations for Amiloride hydrochloride

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

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

Barbaro (2017) Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension. Cell Rep 21 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

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

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