APETx2

• Description:

  APETx2 is a toxin that was originally isolated from Anthopleura elegantissima (Sea anemone) . APETx2 selectively blocks the H (+) -gated sodium channel ASIC3 (ACCN3) . The blockage is rapid and reversible. This toxin does not block isoform ASIC1a (unlike Psalmotoxin 1) and isoform ASIC1b of ASIC1 (ACCN2), nor ASIC2 (ACCN1) . 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.

• Specifications:

  ASIC3 selective inhibitor

• Target:

  ASIC channels

• Sequence:

  GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD

• Peptide Number:

  07APE002

• Disulfide Bonds:

  Cys4-Cys37; Cys6-Cys30; Cys20-Cys38

• N Terminal Sequence:

  H

• C Terminal Sequence:

  OH

• CAS Number:

  713544-47-9