Spadin
Biological Activity
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.
Technical Data
| M. Wt | 2012.34 |
| Formula | C96H142N26O22 |
| Sequence | YAPLPRWSGPIGVSWGLR |
| Storage | Store at -20°C |
| 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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 2012.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.5 mL | 2.48 mL | 4.97 mL |
| 5 mM | 0.1 mL | 0.5 mL | 0.99 mL |
| 10 mM | 0.05 mL | 0.25 mL | 0.5 mL |
| 50 mM | 0.01 mL | 0.05 mL | 0.1 mL |
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References
References are publications that support the products' biological activity.
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.
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Keywords: Spadin, supplier, potent, TREK-1, channels, inhibits, inhibitors, depression, antidepressants, CREB, neurotensin, receptors, NTSR3, gp95, sortilin, K2P, KCNK2, Two-P, Potassium, Channels, Tocris Bioscience
Citations for Spadin
Citations are publications that use Tocris products.
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