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Submit ReviewAPETx2
说明： ASIC3 channel blocker
纯度： ≥95% (HPLC)
生物活性 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 NaV1.8 and NaV1.2 channels (IC50 values are 55 and 114 nM respectively). Demonstrates analgesic properties against acid-induced and inflammatory pain.
技术数据 for APETx2
| 分子量 | 4561.06 |
| 公式 | C196H280N54O61S6 |
| 序列 |
GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD (Modifications: Disulfide bridges: 4-37, 6-30, 20-38) |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for APETx2
| 溶解性 | Soluble to 5 mg/ml in water |
产品说明书 for APETx2
参考文献 for APETx2
参考文献是支持产品生物活性的出版物。
Xiong et al (2008) Acid-sensing ion channels (ASICs) as pharmacological targets for neurodegenerative diseases. Curr.Opin.Pharmacol. 8 25 PMID: 17945532
Karczewski et al (2010) Reversal of acid-induced and inflammatory pain by the selective ASIC3 inhibitor, APETx2. Br.J.Pharmacol. 161 950 PMID: 20860671
Diochot et al (2004) A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons. EMBO J. 23 1516 PMID: 15044953
Blanchard et al (2012) Inhibition of voltage-gated Na(+) currents in sensory neurones by the sea anemone toxin APETx2. Br.J.Pharmacol. 165 2167 PMID: 21943094
Peigneur et al (2012) A natural point mutation changes both target selectivity and mechanism of action of sea anemone toxins. FASEB J. 26 5141 PMID: 22972919
If you know of a relevant reference for APETx2, please let us know.
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关键词: APETx2, APETx2 supplier, acid-sensing, ion, channels, ASIC3, ASIC, blockers, sodium, NaV, 1.8, analgesic, inflammatory, pain, selective, venoms, Voltage-gated, Sodium, Channels, 4804, Tocris Bioscience
2 篇 APETx2 的引用文献
引用文献是使用了 Tocris 产品的出版物。 APETx2 的部分引用包括：
Koei et al (2019) Thin-fibre receptors expressing acid-sensing ion channel 3 contribute to muscular mechanical hypersensitivity after exercise. Eur J Pain 23 1801-1813 PMID: 31314951
Tong et al (2023) Acid-sensing ion channel 3 is required for agmatine-induced histamine-independent itch in mice. Front Mol Neurosci 16 1086285 PMID: 36937045
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