Biological Activity
Potent and selective somatostatin sst4 receptor agonist. Ki values are 0.7, 199, 4720, 1280 and 3880 nM for cloned human sst4, sst1, sst2, sst3 and sst5 receptors respectively. Facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice in vivo.
Technical Data
| M. Wt | 599.56 |
| Formula | C25H29F2N5O3.CF3CO2H |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 217480-26-7 |
| PubChem ID | 45073436 |
| InChI Key | IIRYZHRNVKQVGQ-BDQAORGHSA-N |
| Smiles | FC(F)(F)C(O)=O.NC(NCCC[C@@H]([C@@](OC)=O)NC(CCCC1=C(C3=CC=CC=C3)NC2=C1C=C(F)C=C2F)=O)=N |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 59.96 | 100 | |
| ethanol | 59.96 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 599.56. 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 | 1.67 mL | 8.34 mL | 16.68 mL |
| 5 mM | 0.33 mL | 1.67 mL | 3.34 mL |
| 10 mM | 0.17 mL | 0.83 mL | 1.67 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
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References
References are publications that support the products' biological activity.
Rohrer et al (1998) Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science 282 737 PMID: 9784130
Rohrer and Schaeffer (2000) Identification and characterization of subtype selective somatostatin receptor agonists. J.Physiol.Paris 94 211 PMID: 11087999
Moneta et al (2002) Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice. Eur.J.Neurosci. 16 843 PMID: 12372020
Keywords: L-803,087 trifluoroacetate, supplier, Potent, selective, sst4, agonists, Receptors, Somatostatin, L803087, Somatostatin, Receptors, Somatostatin, Receptors, Tocris Bioscience
