SB 224289 hydrochloride

Name: SB 224289 hydrochloride
Brand: Tocris Bioscience
SKU: 1221
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1221

(1)

Citations (6)

COA / SDS

Selective 5-HT1B antagonist

Key Product Details

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)
Molecular Weight:	557.09

View Full Technical Details for SB 224289 hydrochloride

Technical Data
Citations / Reviews (1)

Biological Activity for SB 224289 hydrochloride

SB 224289 hydrochloride is a 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 for SB 224289 hydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for SB 224289 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	5.57	10 with gentle warming

Preparing Stock Solutions for SB 224289 hydrochloride

The following data is based on the product molecular weight 557.09.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	17.95 mL	89.75 mL	179.50 mL
0.5 mM	3.59 mL	17.95 mL	35.90 mL
1 mM	1.80 mL	8.98 mL	17.95 mL
5 mM	0.36 mL	1.80 mL	3.59 mL

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References for SB 224289 hydrochloride

References are publications that support the biological activity of the product.

Selkirk SB-224289 - a novel selective (human) 5-HT_1B receptor antagonist with negative intrinsic activity. Br.J.Pharmacol. 1998 PMID: 9776361
Hagan Stimulation of 5-HT_1B receptors causes hypothermia in the guinea-pig. Eur.J.Pharmacol. 1997 PMID: 9274976
Roberts Differential effects of 5-HT_1B/1D receptor antagonists in dorsal and median raphe innervated brain regions. Eur.J.Pharmacol. 1998 PMID: 9652357
Gaster The selective 5-HT1B 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. 1998 PMID: 9548813