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APETx2

CAT: 0466-07APE002-00500Size: 0.5 mgDry Ice: NoHazardous: No
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CAT#:0466-07APE002-00500Size:0.5 mg
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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.
CAS Number
713544-47-9
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

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