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Tocris/SB 224289 hydrochloride/1221/10/10 mg

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货号: 1221/10

品牌: Tocris

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Description: Selective 5-HT_1B antagonist

Chemical Name: 1'-Methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine hydrochloride

Purity: ≥95% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Selective 5-HT_1B receptor antagonist (pK_i = 8.2). Displays > 60-fold selectivity over 5-HT_1D, 5-HT_1A, 5-HT_1E, 5-HT_1F, 5-HT_2A and 5-HT_2C receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo.

Licensing Information

Sold with the permission of GlaxoSmithKline

Technical Data

M. Wt	557.09
Formula	C₃₂H₃₂N₄O₃.HCl
Storage	Store at -20°C
Purity	≥95% (HPLC)
CAS Number	180084-26-8
PubChem ID	11226716
InChI Key	GKGKBZYMDILCOF-UHFFFAOYSA-N
Smiles	O=C(C5=CC=C(C6=CC=C(C7=NOC(C)=N7)C=C6C)C=C5)N2C1=CC3=C(OCC43CCN(CC4)C)C=C1CC2.Cl

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	5.57	10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 557.09. 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	1.8 mL	8.98 mL	17.95 mL
5 mM	0.36 mL	1.8 mL	3.59 mL
10 mM	0.18 mL	0.9 mL	1.8 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Gaster et al (1998) The selective 5-HT_1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine (SB-224289) potently blocks terminal 5-HT J.Med.Chem. 41 1218 PMID: 9548813

Hagan et al (1997) Stimulation of 5-HT_1B receptors causes hypothermia in the guinea-pig. Eur.J.Pharmacol. 331 169 PMID: 9274976

Roberts et al (1998) Differential effects of 5-HT_1B/1D receptor antagonists in dorsal and median raphe innervated brain regions. Eur.J.Pharmacol. 346 175 PMID: 9652357

Selkirk et al (1998) SB-224289 - a novel selective (human) 5-HT_1B receptor antagonist with negative intrinsic activity. Br.J.Pharmacol. 125 202 PMID: 9776361

Keywords: SB 224289 hydrochloride, supplier, Selective, 5-HT1B, antagonist, Serotonin, Receptors, SB224289, hydrochloride, GlaxoSmithKline, GSK, 5-HT1B, Receptors, 5-HT1B, Receptors, Tocris Bioscience

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