APETx2
Purity: ≥95%
Biological Activity
APETx2 is an acid-sensing ion channel 3 (ASIC3) channel blocker (IC50 values are 63 and 175 nM for homomeric rat and human ASIC3 channels). Also inhibits NaV1.8 and NaV1.2 channels (IC50 values are 55 and 114 nM respectively). Demonstrates analgesic properties against acid-induced and inflammatory pain.Technical Data
(Modifications: Disulfide bridges: 4-37, 6-30, 20-38)
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.
Background References
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Acidic pH promotes intervertebral disc degeneration: Acid-sensing ion channel -3 as a potential therapeutic target
Sci Rep, 2016;6(0):37360. -
A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins.
Peigneur et al.
FASEB J., 2012;26:5141 -
Acid-sensing ion channels (ASICs) as pharmacological targets for neurodegenerative diseases.
Xiong et al.
Curr.Opin.Pharmacol., 2008;8:25 -
Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2.
Karczewski et al.
Br.J.Pharmacol., 2010;161:950 -
A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons.
Diochot et al.
EMBO J., 2004;23:1516 -
Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2.
Blanchard et al.
Br.J.Pharmacol., 2012;165:2167
Product Datasheets
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Citations for APETx2
The citations listed below are publications that use Tocris products. Selected citations for APETx2 include:
2 Citations: Showing 1 - 2
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Acid-sensing ion channel 3 is required for agmatine-induced histamine-independent itch in mice.
Authors: Tong Et al.
Front Mol Neurosci 2023;16:1086285
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Thin-fibre receptors expressing acid-sensing ion channel 3 contribute to muscular mechanical hypersensitivity after exercise.
Authors: Koei Et al.
Eur J Pain 2019;23:1801-1813
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