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Description: ASIC3 channel blocker
Purity: ≥95% (HPLC)
Biological Activity for APETx2
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 for APETx2
| M. Wt | 4561.06 |
| Formula | C196H280N54O61S6 |
| Sequence |
GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD (Modifications: Disulfide bridges: 4-37, 6-30, 20-38) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 713544-47-9 |
| PubChem ID | 90488973 |
| InChI Key | HEHYILNFEUDIQC-UHFFFAOYSA-N |
| Smiles | [H]NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CO)NC1=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CC1=CNC4=C1C=CC=C4)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CSSC[C@H](NC2=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CC(O)=O)C(O)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N3)[C@@H](C)O |
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 APETx2
| Solubility | Soluble to 5 mg/ml in water |
Product Datasheets for APETx2
References for APETx2
References are publications that support the biological activity of the product.
Xiong et al (2008) Acid-sensing ion channels (ASICs) as pharmacological targets for neurodegenerative diseases. Curr.Opin.Pharmacol. 8 25 PMID: 17945532
Karczewski et al (2010) Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2. Br.J.Pharmacol. 161 950 PMID: 20860671
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
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
If you know of a relevant reference for APETx2, please let us know.
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Keywords: APETx2, APETx2 supplier, acid-sensing, ion, channels, ASIC3, ASIC, blockers, sodium, NaV, 1.8, analgesic, inflammatory, pain, selective, venoms, Voltage-gated, Sodium, Channels, 4804, Tocris Bioscience
2 Citations for APETx2
Citations are publications that use Tocris products. Selected citations for APETx2 include:
Koei et al (2019) Thin-fibre receptors expressing acid-sensing ion channel 3 contribute to muscular mechanical hypersensitivity after exercise. Eur J Pain 23 1801-1813 PMID: 31314951
Tong et al (2023) Acid-sensing ion channel 3 is required for agmatine-induced histamine-independent itch in mice. Front Mol Neurosci 16 1086285 PMID: 36937045
Do you know of a great paper that uses APETx2 from Tocris? Please let us know.
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