APETx2

Pricing Availability   Qty
Description: ASIC3 channel blocker
Purity: ≥95% (HPLC)
Datasheet
Citations (2)
Reviews

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

Certificate of Analysis / Product Datasheet
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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:

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

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


Do you know of a great paper that uses APETx2 from Tocris? Please let us know.

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