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Tocris/LY 393558/3350/50/50 mg

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货号: 3350/50

品牌: Tocris

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Description: Dual 5-HT_1B/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)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Dual 5-HT_1B/1D receptor antagonist (pK_B 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-HT_2A and 5-HT_2B receptors (pK_i 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
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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Mitchell et al (2001) LY393558, a 5-hydroxytryptamine reuptake inhibitor and 5-HT_1B/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-HT_1B/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

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