LY 393558

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Cat.No. 3350 - LY 393558 | C26H31FN4O4S2 | CAS No. 271780-64-4
Description: Dual 5-HT1B/1D antagonist and 5-HT re-uptake inhibitor
Chemical Name: 1-[2-[4-(6-Fluoro-1H-indol-3-yl)-3,6-dihydro-1(2H)-pyridinyl]ethyl]-3,4-dihydro-3-(1-methylethyl)-6-(methylsulfonyl)-1H-2,1,3-benzothiadiazine-2,2-dioxide
Purity: ≥97% (HPLC)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

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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


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Keywords: 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

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