Biological ActivityAPETx2 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.
(Modifications: Disulfide bridge between 4-37, 6-30, 20-38)
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2.
Karczewski et al.
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.
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