Spadin

Pricing Availability Delivery Time Qty
Cat.No. 5594 - Spadin | Tyr-Ala-Pro-Leu-Pro-Arg-Trp-Ser-Gly-Pro-Ile-Gly-Val-Ser-Trp-Gly-Leu-Arg | CAS No. 1270083-24-3
Description: Potent K2P2.1 (TREK-1) channel blocker
Datasheet
Citations
Literature

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

SolubilitySoluble 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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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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, Two-P, Potassium, Channels, Tocris Bioscience

Citations for Spadin

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