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Submit ReviewSpadin is a potent TREK-1 channel blocker (IC50 = 71 nM). Enhances dorsal raphe nucleus 5-HT neurotransmission in mice. Induces hippocampal CREB activation and neurogenesis in adult mice. Exhibits antidepressant effects in mouse models of depression. Brain penetrant.
分子量 | 2012.34 |
公式 | C96H142N26O22 |
序列 | YAPLPRWSGPIGVSWGLR |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 1270083-24-3 |
PubChem ID | 91826106 |
InChI Key | WMSPWLIEKXALQP-WSSJNERPSA-N |
Smiles | [H]N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CO)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=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。
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溶解性 | Soluble to 2 mg/ml in water |
参考文献是支持产品生物活性的出版物。
Mazella et al (2010) Spadin, a sortilin-derived peptide, targeting rodent TREK-1 channels: a new concept in the antidepressant drug design. PLoS Biol. 8 e1000355 PMID: 20405001
Borsotto et al (2015) Targeting two-pore domain K(+) channels TREK-1 and TASK-3 for the treatment of depression: a new therapeutic concept. Br.J.Pharmacol. 172 771 PMID: 25263033
If you know of a relevant reference for Spadin, please let us know.
关键词: Spadin, Spadin supplier, potent, TREK-1, channels, inhibits, inhibitors, depression, antidepressants, CREB, neurotensin, receptors, NTSR3, gp95, sortilin, K2P, KCNK2, Two-P, Potassium, Channels, 5594, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Spadin 的部分引用包括:
Fernandez-Fernandez et al (2018) Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons. PLoS One 13 e0199282 PMID: 29928032
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平均评分: 5 (Based on 1 Review.)
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A very potent K2p channel blocker which was used to figure out the blocking activity as concentration of the blocker molecule increased. Spadin is a great antagonist molecule which shows channel blocking properties which is concentration dependent.