Toxin APETx2
A Blocker of ASIC3 Channel
Cat #: STA-160
Sizes: 0.1 mg, 0.5 mg, 1 mg, 5 mg
Source: Synthetic
MW: 4561 Da.
Net Peptide Content: 100%
Target: ASIC3 channels
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Natural APETx2 is a 42-amino-acid peptidyl toxin, originally isolated from the sea anemone Anthopleura elegantissima. APETx2 was shown to be a selective, potent and reversible blocker of the homodimer proton gated channel ASIC3. ASIC3 has been implicated in pain transduction associated with acidosis in inflamed or ischemic tissues. APETx2 directly inhibits the ASIC3 channel by acting at its external side of the channel in a pH dependent manner.
APETx2 also inhibits the hetromer ASIC2b-ASIC3 channel but does not inhibit the activity of ASIC1 isoform1.
Structurally APETx2 is related to APETx1 a toxin that targets HERG K+ channel1,2.
Alomone Labs is pleased to offer APETx2 (#STA-160), a synthetic peptide.
References
Diochot, S. et al. (2004) EMBO J. 23, 1516.
Chagot, B. et al. (2005) Protein Sci. 14, 2003.
Gao, M. et al. (2016) Eur. J. Ortho.38, 577.
Yan, J. et al. (2013) Headache53, 1250.
Izumi, M. et al. (2012) J. Biomed. Sci.19, 77.
For a list of product citations in the literature, see product citations tab below. If you know of additional relevant citations for this product, please let us know.
Our Bioassay
Specifications
Citations
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Our bioassay
Alomone Labs APETx2 inhibits Asic3 channels expressed in Xenopus oocytes. A.Time course of APETx2 (#STA-160)inhibition of Asic3 channels current. Membrane potential was held at -60 mV, current was elicited every 50 sec by a transient applications of pH 5.5, and was inhibited significantly by 4 min applications of 0.5 µM and 1 µM APETx2, as indicated by horizontal bars.
B.Superimposed traces of Asic3 currents upon application of control, 0.5 µM and 1 µM APETx2 (taken from the experiment in A).
OriginAnthopleura elegantissima (Sea anemone).
Purity>98%.
Effective concentration10 nM - 3 µM.
SequenceGTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD.
ModificationsDisulfide bonds between Cys4-Cys37, Cys6-Cys30 and Cys20-Cys38.
Molecular formulaC196H280N54O61S6.
CAS number713544-47-9.
ActivityAPETx2 inhibits ASIC3 channels1.
Storage before reconstitutionLyophilized powder can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
ReconstitutionAny aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitutionUp to one week at 4°C or three months at -20°C.
Product citations