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.
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- CAS No.: 713544-47-9
- Formule: C196H280N54O61S6
- Masse moléculaire:4561.00
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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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Masse moléculaire 4561.00
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvant et solubilité
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. |
Pureté et documentation
Références
[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)
APETx2 Related Classifications
HY-P1346 Related Classifications
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