Cat. No. 4804
Biological ActivityAcid-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)
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Blanchard et al (2012) Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2. Br.J.Pharmacol. 165 2167. PMID: 21943094.
Peigneur et al (2012) A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins. FASEB J. 26 5141. PMID: 22972919.
Karczewski et al (2010) Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2. Br.J.Pharmacol. 161 950. PMID: 20860671.
Xiong et al (2008) Acid-sensing ion channels (ASICs) as pharmacological targets for neurodegenerative diseases. Curr.Opin.Pharmacol. 8 25. PMID: 17945532.
Diochot et al (2004) A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons. EMBO J. 23 1516. PMID: 15044953.
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Keywords: APETx2, supplier, acid-sensing, ion, channels, ASIC3, ASIC, channels, blockers, sodium, NaV, 1.8, analgesic, inflammatory, pain, selective, venoms, Tocris Bioscience, Acid-Sensing Ion Channel Blocker products
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