APETx2 (0.1 mg vial)

Product overview
Catalog Number
PPH08-0156
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
Target
Selective Blocker of Acid-Sensing Ion Channel, ASIC3, A synthetic sea anenome toxin
Description
This toxin potently blocks acid-sensing ion channel ASIC3 homotrimers and heterotrimers containing ASIC3 (composed with isoforms of ASIC1 and ASIC2) (PubMed:15044953). It also weakly inhibits potassium channels, and sodium channels (PubMed:15044953, PubMed:21943094, PubMed:22972919, PubMed:25337890). On homomeric ASIC3, this protein shows IC50=57-87 nM on rat, 37.3 nM on mouse and 175 nM on human channels (PubMed:15044953, PubMed:18923424, PubMed:19306891, PubMed:20813121, PubMed:21943094, PubMed:22851922, PubMed:22851929). The blockade is rapid and reversible (PubMed:15044953). On heterotrimeric forms, the toxin is less potent (IC50=117 nM on rat ASIC2b-ASIC3 channel, 900 nM on rat ASIC1b-ASIC3, and 2 µM on rat ASIC1a-ASIC3) (PubMed:15044953). It weakly inhibits Kv3.4/KCNC4 potassium channels (3 µM of the toxin inhibits 38% of Kv3.4 current) (PubMed:15044953). It reversibly and voltage-dependently inhibits hKv11.1/KCNH2/ERG1 potassium channels (IC50=1.21 µM), inhibiting both peak and tail currents without action on channel inactivation (PubMed:25337890). It weakly inhibits rNav1.2/SCN2A (EC(50)=114 nM), rNav1.6/SCN8A current (17% at 1 µM of the toxin) and Nav1.8/SCN10A (IC50=6.6 µM on human channels expressed in oocytes, EC(50)=55 nM on rat channels expressed in oocytes, and 2.6 µM on rat channels in DRG neurons) (PubMed:21943094, PubMed:22972919). It may act on sodium channels by binding at site 1 or close by, when the pore is in an open configuration (PubMed:22972919). In vivo, central injection does not induce neurotoxin symptoms in mice even after 24 hours (PubMed:15044953). However, it abolishes acid-induced pain in rats
Category
Catalog peptides, Biologically Active Peptides
Product Properties
Quantity

1mg
Storage

Shipped at 4°C. Store at -20°C for one year.
Purity

> 95%
Source

Synthetic
Forma appearance

Lyophilized powder
Price

€240.00
  • For research use only
  • Not for use in diagnostic procedures

€240,00 Tax excluded
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