APETx2
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.
For research use only. We do not sell to patients.
- CAS No.: 713544-47-9
- Formula: C196H280N54O61S6
- Molecular Weight:4561.00
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
APETx2 (i.t. or i.m. application, 0.022 to 2.2 µM) resulted in a potent and complete reversal of established mechanical hypersensitivity in the complete Freund's adjuvant (CFA) inflammatory pain model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 713544-47-9
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Molecular Weight 4561.00
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Formula C196H280N54O61S6
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Sequence
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 (Disulfide bridge:Cys4-Cys37;Cys6-Cys30;Cys20-Cys38)
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Sequence Shortening
GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD (Disulfide bridge:Cys4-Cys37;Cys6-Cys30;Cys20-Cys38)
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Structure Classification
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Initial Source
Anthopleura elegantissima
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
H2O
Peptide Solubility and Storage Guidelines:
1. Calculate the length of the peptide.
2. Calculate the overall charge of the entire peptide according to the following table:
| Contents | Assign value | |
| Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 |
| Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 |
| Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution:
| Overall charge of peptide | Details |
| Negative (<0) |
1. Try to dissolve the peptide in water first. 2. If water fails, add NH4OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. |
| Positive (>0) |
1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. |
| Zero (=0) |
1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
Purity & Documentation
References
[1]. Sylvie Diochot, et al. A New Sea Anemone Peptide, APETx2, Inhibits ASIC3, a Major Acid-Sensitive Channel in Sensory Neurons. EMBO J. 2004 Apr 7;23(7):1516-25. [Content Brief]
[2]. Jerzy Karczewski, et al. Reversal of Acid-Induced and Inflammatory Pain by the Selective ASIC3 Inhibitor, APETx2. Br J Pharmacol. 2010 Oct;161(4):950-60. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)