APETx2

Pricing Availability Delivery Time Qty
Cat.No. 4804 - APETx2 | Gly-Thr-Ala-Cys-Ser-Cys-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-ser-Cys-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys-Arg-Tyr-Phe-Leu-Gly-Thr-Cys-Cys-Thr-Pro-Ala-Asp | CAS No. 713544-47-9
Description: ASIC3 channel blocker
Datasheet
Citations
Literature

Biological Activity

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

M. Wt 4561.06
Formula C196H280N54O61S6
Sequence GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD

(Modifications: Disulfide bridge between 4-37, 6-30, 20-38)

Storage Store at -20°C
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 5 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 4561.06. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.22 mL 1.1 mL 2.19 mL
5 mM 0.04 mL 0.22 mL 0.44 mL
10 mM 0.02 mL 0.11 mL 0.22 mL
50 mM 0 mL 0.02 mL 0.04 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: APETx2, supplier, acid-sensing, ion, channels, ASIC3, ASIC, channels, blockers, sodium, NaV, 1.8, analgesic, inflammatory, pain, selective, venoms, ASIC, Tocris Bioscience

Citations for APETx2

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Literature in this Area

Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

Pathways for APETx2

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