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Submit ReviewAmiloride hydrochloride
Description: Na+ channel blocker; also I2 imidazoline ligand
Chemical Name: 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride
Purity: ≥98% (HPLC)
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 |
| 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 Data 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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Product Datasheets for Amiloride hydrochloride
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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Keywords: Amiloride hydrochloride, Amiloride hydrochloride supplier, I2, selective, ligands, differentiates, I2A, I2B, Na+, channel, blockers, Imidazoline, Receptors, Sodium, NaV, Channels, voltage-gated, voltage-dependent, NHE, H+, exchanger, ASIC, upa, urokinase-type, plasminogen, inhibitors, inhibits, Voltage-gated, Na+/H+, Exchanger, TRPP, Urokinase, 0890, Tocris Bioscience
7 Citations for Amiloride hydrochloride
Citations are publications that use Tocris 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
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
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
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.
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.