| 货号 | 4804/100U |
| 供应商 | Tocris |
| 生物活性 | Acid-sensing ion channel 3 (ASIC3) channel blocker (IC50 values are 63 and 175 nM for homomeric rat and human ASIC3 channels). Also inhibits NaV1.8 and NaV1.2 channels (IC50 values are 55 and 114 nM respectively). Demonstrates analgesic properties against acid-induced and inflammatory pain. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 计算分子量 | 4561.06 |
| 分子式 | C196H280N54O |
| 可溶性/溶解性 | Soluble to 5 mg/ml in water |
| 序列号 | GTACSCGNSKGIYWFYRPSCPTDRGYTGSC (Modifications: Disulfide bridge between 4-37, 6-30, 20-38) |
| 参考文献 | Blanchardet al (2012) Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2. Br.J.Pharmacol. 165 2167. PMID: 21943094. Peigneuret al (2012) A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins. FASEB J. 26 5141. PMID: 22972919. Karczewskiet al (2010) Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2. Br.J.Pharmacol. 161 950. PMID: 20860671. Xionget al (2008) Acid-sensing ion channels (ASICs) as pharmacological targets for neurodegenerative diseases. Curr.Opin.Pharmacol. 8 25. PMID: 17945532. Diochotet al (2004) A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons. EMBO J. 23 1516. PMID: 15044953. |