APETx2
Product ID L8525 
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 x 100µg 140.00

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5 x 100µg 560.00

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For quotation of big quantities, please Contact us
 Product Technical Documents
Safety Data Sheet Available on request, please Contact us
Ref. SDS_L8525 : unit price : free of charge
 Chemical and Physical Properties
Product code L8525  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


 
Savety Recommandations  
 Bibliographic References
Product code L8525 
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
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