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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||2.66||10 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|
References are publications that support the biological activity of the product.
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
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
3 Citations for Amiloride hydrochloride
Citations are publications that use Tocris products. Selected citations for Amiloride hydrochloride include:
Barbaro (2017) Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension. Cell Rep 21 1009 PMID: 29069584
Jeong et al (2013) Antinociceptive effects of amiloride and benzamil in neuropathic pain model rats. Int J Nanomedicine 28 1238 PMID: 23960454
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? Please let us know.
Reviews for Amiloride hydrochloride
Average Rating: 3 (Based on 1 Review.)
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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.
Literature in this Area
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.