Biological Activity
Dual 5-HT1B/1D receptor antagonist (pKB values are 9.05 and 8.98 respectively) and 5-HT re-uptake inhibitor (pIC50 = 8.48). Potently antagonizes terminal autoreceptor activity in vitro and increases extracellular 5-HT levels above those evoked by fluoxetine (Cat. No. 0927) in vivo. Also acts as an antagonist at 5-HT2A and 5-HT2B receptors (pKi values are 7.29 and 7.35 respectively).
Technical Data
| M. Wt | 546.68 |
| Formula | C26H31FN4O4S2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 271780-64-4 |
| PubChem ID | 10347428 |
| InChI Key | QUSLYAPLTMMCFE-UHFFFAOYSA-N |
| Smiles | CC(C)N2S(N(CCN3CC=C(C4=CNC5=C4C=CC(F)=C5)CC3)C1=CC=C(S(=O)(C)=O)C=C1C2)(=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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.67 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 546.68. 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 | 1.83 mL | 9.15 mL | 18.29 mL |
| 5 mM | 0.37 mL | 1.83 mL | 3.66 mL |
| 10 mM | 0.18 mL | 0.91 mL | 1.83 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Mitchell et al (2001) LY393558, a 5-hydroxytryptamine reuptake inhibitor and 5-HT1B/1D receptor antagonist: effects on extracellular levels of 5-hydroxytryptamine in the guinea pig and rat. Eur.J.Pharmacol. 432 19 PMID: 11734183
Pullar et al (2001) In vitro activity of LY393558, an inhibitor of the 5-hydroxytryptamine transporter with 5-HT1B/1D/2 receptor antagonist properties. Eur.J.Pharmacol. 432 9 PMID: 11734182
Morecroft et al (2005) Functional interactions between 5-hydroxytryptamine receptors and the serotonin transporter in pulmonary arteries. J.Pharmacol.Exp.Ther. 313 539 PMID: 15659538
Keywords: LY 393558, supplier, LY393558, dual, 5-HT1B, 5-HT1D, 5-HT1B/1D, receptors, antagonists, serotonin, reuptake, uptake, SERT, inhibitors, inhibits, transporters, 5-HT1, 5-Hydroxytryptamine, 5-HT1B, Receptors, 5-HT1D, Receptors, 5-HT, Transporters, 5-HT1B, Receptors, Tocris Bioscience
