APETx2 

APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC₅₀ of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain^[1][2].

APETx2 (i.t. or i.m. application, 0.022 to 2.2 µM) resulted in a potent and complete reversal of established mechanical hypersensitivity in the complete Freund's adjuvant (CFA) inflammatory pain model^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

4561.00

C₁₉₆H₂₈₀N₅₄O₆₁S₆

713544-47-9

Gly-Thr-Ala-Cys-Ser-Cys-Gly-Asn-Ser-Lys-Gly-Ile-Tyr-Trp-Phe-Tyr-Arg-Pro-Ser-Cys-Pro-Thr-Asp-Arg-Gly-Tyr-Thr-Gly-Ser-Cys-Arg-Tyr-Phe-Leu-Gly-Thr-Cys-Cys-Thr-Pro-Ala-Asp (Disulfide bridge:Cys4-Cys37;Cys6-Cys30;Cys20-Cys38)

GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD (Disulfide bridge:Cys4-Cys37;Cys6-Cys30;Cys20-Cys38)

O=C(N[C@@H]([C@H](O)C)C(N[C@@H](C)C(N[C@@H](CSSC[C@@H]1NC2=O)C(N[C@@H](CO)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC3=CC=C(C=C3)O)C(N[C@@H](CC4=CC=CC=C4)C(N[C@@H](CC(C)C)C(NCC(N[C@H]2[C@H](O)C)=O)=O)=O)=O)=O)=O)NC5=O)C(NCC(N[C@@H](CC(N)=O)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(NCC(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC6=CC=C(C=C6)O)C(N[C@@H](CC7=CNC8=CC=CC=C78)C(N[C@@H](CC9=CC=CC=C9)C(N[C@@H](CC%10=CC=C(C=C%10)O)C(N[C@@H](CCCNC(N)=N)C(N%11[C@@H](CCC%11)C(N[C@@H](CO)C(N[C@@H](CSSC[C@@H](C(N[C@@H]([C@H](O)C)C(N%12[C@@H](CCC%12)C(N[C@@H](C)C(N[C@@H](CC(O)=O)C(O)=O)=O)=O)=O)=O)NC1=O)C(N%13[C@@H](CCC%13)C(N[C@@H]([C@H](O)C)C(N[C@@H](CC(O)=O)C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@@H](CC%14=CC=C(C=C%14)O)C(N[C@@H]([C@H](O)C)C(NCC(N[C@H]5CO)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CN

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Sylvie Diochot, et al. A New Sea Anemone Peptide, APETx2, Inhibits ASIC3, a Major Acid-Sensitive Channel in Sensory Neurons. EMBO J. 2004 Apr 7;23(7):1516-25.  [Content Brief]

  [2]. Jerzy Karczewski, et al. Reversal of Acid-Induced and Inflammatory Pain by the Selective ASIC3 Inhibitor, APETx2. Br J Pharmacol. 2010 Oct;161(4):950-60.  [Content Brief]