| Bioactivity | APETx2 TFA, 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]. |
| In Vivo | 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]. |
| Name | APETx2 TFA |
| Sequence | 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) |
| Shortening | GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD (Disulfide bridge:Cys4-Cys37;Cys6-Cys30;Cys20-Cys38) |
| Formula | C198H281F3N54O62S6 |
| Molar Mass | 4675.02 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. |