| CAS | 713544-47-9 |
| Sequence | H-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-OH(Disulfide bridge between 4-37, 6-30, 20-38) |
| Sequence Single | GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD(Disulfide bridge between 4-37, 6-30, 20-38) |
| Molecular Formula | C196H280N54O61S6 |
| Molecular Weight | 4561.06 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Description | 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). APETx2 also inhibits NaV1.8 and NaV1.2 channels (IC50 values are 55 and 114 nM respectively). APETx2 demonstrates analgesic properties against acid-induced and inflammatory pain. |
| References | 1. Acid-sensing ion channels (ASICs) as pharmacological targets for neurodegenerative diseases. Xiong et al (2008). Curr.Opin.Pharmacol. 8 25 PMID: 17945532 2. Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2. Karczewski et al (2010). Br.J.Pharmacol. 161 950 PMID: 20860671 3. A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons. Diochot et al (2004). EMBO J. 23 1516 PMID: 15044953 4. Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2. Blanchard et al (2012). Br.J.Pharmacol. 165 2167 PMID: 21943094 5. A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins. Peigneur et al (2012). FASEB J. 26 5141 PMID: 22972919 |