APETx2

Name APETx2
Supplier Tocris Bioscience
Catalog 2427
Prices $319.00
Sizes 100 µg
Function Type Blocker
Cas Number 713544-47-9
Formula C196H280N54O61S6
Molecular Weight 4561.06
Description Acid-sensing ion channel 3 (ASIC3) channel blocker (IC 50 values are 63 and 175 nM for homomeric rat and human ASIC3 channels). Also inhibits Na V 1.8 and Na V 1.2 channels (IC 50 values are 55 and 114 nM respectively). Demonstrates analgesic properties against acid-induced and inflammatory pain.
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Product References

A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel - A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel

Diochot S, Baron A, Rash LD, Deval E, Escoubas P, Scarzello S, Salinas M, Lazdunski M. EMBO J. 2004 Apr 7;23(7):1516-25. Epub 2004 Mar 25.

Acid-sensing ion channels (ASICs) as pharmacological targets for - Acid-sensing ion channels (ASICs) as pharmacological targets for

Xiong ZG, Pignataro G, Li M, Chang SY, Simon RP. Curr Opin Pharmacol. 2008 Feb;8(1):25-32. Epub 2007 Oct 22.

Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, - Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor,

Karczewski J, Spencer RH, Garsky VM, Liang A, Leitl MD, Cato MJ, Cook SP, Kane S, Urban MO. Br J Pharmacol. 2010 Oct;161(4):950-60.

Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone - Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone

Blanchard MG, Rash LD, Kellenberger S. Br J Pharmacol. 2012 Apr;165(7):2167-77.

A natural point mutation changes both target selectivity and mechanism of action - A natural point mutation changes both target selectivity and mechanism of action

Peigneur S, Beress L, Moller C, Mari F, Forssmann WG, Tytgat J. FASEB J. 2012 Dec;26(12):5141-51.