TargetMol

APETx2

Product Code:
 
TAR-TP2081
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-TP2081-10mg10mg£2,184.00
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Further Information

Bioactivity:
Acid-sensing ion channel 3 (ASIC3) channel blocker (IC50 values are 63 and 175 nM for homomeric rat and human ASIC3 channels). Also inhibits NaV1.8 and NaV1.2 channels (IC50 values are 55 and 114 nM respectively). Demonstrates analgesic properties against acid-induced and inflammatory pain.
CAS:
713544-47-9
Formula:
C196H280N54O61S6
Molecular Weight:
4561.06
Purity:
0.98
SMILES:
0

References

Xiong et al (2008) Acid-sensing ion channels (ASICs) as pharmacological targets for neurodegenerative diseases. Curr.Opin.Pharmacol. 8 25 PMID: Karczewski et al (2010) Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2. Br.J.Pharmacol. 161 950 PMID: Blanchard et al (2012) Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2. Br.J.Pharmacol. 165 2167 PMID: Diochot et al (2004) A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons. EMBO J. 23 1516 PMID: Peigneur et al (2012) A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins. FASEB J. 26 5141 PMID: