APETx2

Name: APETx2
Brand: Tocris Bioscience
SKU: 4804

Tocris Bioscience, part of Bio-Techne | Catalog # 4804

Citations (9)

COA / SDS

ASIC3 channel blocker

Key Product Details

Description:	ASIC3 channel blocker
Purity:	≥95% (HPLC)
Molecular Weight:	4561.06

View Full Technical Details for APETx2

Technical Data
Citations

Biological Activity for APETx2

APETx2 is an acid-sensing ion channel 3 (ASIC3) channel blocker (IC₅₀ values are 63 and 175 nM for homomeric rat and human ASIC3 channels). Also inhibits Na_V1.8 and Na_V1.2 channels (IC₅₀ values are 55 and 114 nM respectively). Demonstrates analgesic properties against acid-induced and inflammatory pain.

Technical Data for APETx2

M. Wt	4561.06
Formula	C₁₉₆H₂₈₀N₅₄O₆₁S₆
Single Letter Sequence	GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD (Modifications: Disulfide bridges: 4-37, 6-30, 20-38)
Storage	Store at -20°C
Purity	≥95% (HPLC)
CAS Number	713544-47-9
PubChem ID	90488973
InChi Key	HEHYILNFEUDIQC-UHFFFAOYSA-N
Smiles	[H]NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CO)NC1=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CC1=CNC4=C1C=CC=C4)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CSSC[C@H](NC2=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CC(O)=O)C(O)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N3)[C@@H](C)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for APETx2

Solubility

Soluble to 5mg/ml in water

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References for APETx2

References are publications that support the biological activity of the product.

Peigneur A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins. FASEB J. 2012 PMID: 22972919
Blanchard Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2. Br.J.Pharmacol. 2012 PMID: 21943094
Karczewski Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2. Br.J.Pharmacol. 2010 PMID: 20860671
Diochot A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons. EMBO J. 2004 PMID: 15044953
Xiong Acid-sensing ion channels (ASICs) as pharmacological targets for neurodegenerative diseases. Curr.Opin.Pharmacol. 2008 PMID: 17945532