(Syn. : Pi-actitoxin-Ael2b, Pi-AITX-Ael2b)
APETx2 | Product ID | L8525-100UG |
| Name | APETx2 |
| Molecular formula | C196H280N54O61S6 |
| Description |
A 42 amino-acids peptide with 3 disulfide bridges , synthetic, initially isolated from the venom of the Clonal anemone Anthopleura elegantissima. |
| Biological activity | Pi-actitoxin-Ael2b (APETx2) selectively blocks the H(+)-gated sodium channel ASIC3 (ACCN3). The blockage is rapid and reversible. It also inhibits the heteromeric ASIC2b-ASIC3 channel, and has less affinity for ASIC1b-ASIC3, ASIC1a-ASIC3, and no effect on the ASIC2a-ASIC3 channels. IC50 is 63 nM on ASIC3 channel. IC50 is 117 nM on ASIC2b-ASIC3 heteromeric channel. IC50 is 0.9 µM on ASIC1b-ASIC3 heteromeric channel. IC50 is 2 µM on ASIC1a-ASIC3 heteromeric channel. Interestingly, recent studies demonstrated that APETx2 also inhibits Nav1.8 currents with an IC50 of around 2 µM. APETx2 does not block rat ASIC1a and ASIC1b (ASIC1 isoforms), ASIC2a (ASIC2 isoform), and the heteromeric ASIC2a-ASIC3 channels. It also does not inhibit most of voltage-gated potassium channels tested (Kv1.4, Kv2.2, Kv3.1, Kv4.1, Kv4.2, Kv4.3). It does not inhibit Nav1.3, Nav1.4, Nav1.5 and Nav1.7. It shows a very weak inhibition on Nav1.6 (17% inhibition by 1 µM of the toxin). |
Packaging and Prices
| Packaging | Price (€) | Quantité | Buy Now |
|---|---|---|---|
| 1 Unité(s) | 140.00 | ||
| 5 Unité(s) | 560.00 | ||
| For quotation of big quantities, please Contact us | |||
Product Technical Documents
 | Safety Data Sheet Available on request, please Contact us Ref. SDS_L8525-100UG : unit price : free of charge |
Chemical and Physical Properties
| Product code | L8525-100UG | Molecular weight | 4561.13 Da |
| Product name | APETx2 | Physical form | White lyophilized solid |
| CAS No. | NA | Melting point | |
| RTECS | NA | Solubility | water and saline buffer |
| UNIPROT | P61542 | Optical Activity | |
| PubChem SID | |||
| PubChem CID | 90488973 | ||
| Purity | > 98 % | ||
| Toxicity(LD50) | No Data | ||
| Chemical Name | |||
| Storage & Reconstitution Recommandations |
Stable at room temperature, store preferably at 4°C |
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| Savety Recommandations | |||
Bibliographic References
| Product code | L8525-100UG |
| Product name | APETx2 |
- 1. Blanchard MG, Rash LD, Kellenberger S. (2011) Inhibition of voltage-gated Na(+) currents in sensory neurons by the sea anemone toxin APETx2. Br J Pharmacol. PubMed link ;
2. Chagot B., et al. (2005) Solution structure of APETx2, a specific peptide inhibitor of ASIC3 proton-gated channels, Protein Sci. ;
3. Delaunay A., et al. (2012) Human ASIC3 channel dynamically adapts its activity to sense the extracellular pH in both acidic and alkaline directions. PNAS. ;
4. Diochot S., et al. (2004) A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons. EMBO J. ;
5. Peigneur S, et al. (2012) A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins. FASEB J. PubMed link ;
6. Tian, Y., et al. (2017). Glioblastoma cancer stem cell lines express functional acid sensing ion channels ASIC1a and ASIC3. Sci. Rep., 7, 13674. doi: 10.1038/s41598-017-13666-9. PMCID: PMC5651884. ;
7. Tsuchimochi H, Yamauchi K, McCord JL, Kaufman MP. (2011) Blockade of Acid Sensing Ion Channels Attenuates the Augmented Exercise Pressor Reflex in Rats with Chronic Femoral Artery Occlusion. J Physiol. PubMed link
Links
| Product code | L8525-100UG |
| Product name | APETx2 |
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