RS 102221 hydrochloride

Name: RS 102221 hydrochloride
Brand: Tocris Bioscience
SKU: 1050

Tocris Bioscience, part of Bio-Techne | Catalog # 1050

Citations (16)

COA / SDS

Selective 5-HT2C antagonist

Key Product Details

Description:	Selective 5-HT_2C antagonist
Chemical Name:	8-[5-(2,4-Dimethoxy-5-(4-trifluoromethylphenylsulphonamido)phenyl-5-oxopentyl]-1,3,8-triazaspiro[4.5]decane-2,4-dione hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	649.08

View Full Technical Details for RS 102221 hydrochloride

Technical Data
Citations

Biological Activity for RS 102221 hydrochloride

RS 102221 hydrochloride is a potent and selective 5-HT_2C antagonist (pK_i = 8.7). Displays ~ 100-fold selectivity over the 5-HT_2A and 5-HT_2B subtypes and is > 100-fold selective over other 5-HT receptors, α- and β-adrenergic and muscarinic ACh receptors.

Licensing Information

Sold with the permission of Roche Bioscience

Compound Libraries for RS 102221 hydrochloride

RS 102221 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for RS 102221 hydrochloride

M. Wt	649.08
Formula	C₂₇H₃₁F₃N₄O₇S.HCl
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	187397-18-8
PubChem ID	18931299
InChi Key	SZJZEJZLRDIHPB-UHFFFAOYSA-N
Smiles	Cl.COC1=CC(OC)=C(NS(=O)(=O)C2=CC=C(C=C2)C(F)(F)F)C=C1C(=O)CCCCN1CCC2(CC1)NC(=O)NC2=O

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 RS 102221 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO		100

Preparing Stock Solutions for RS 102221 hydrochloride

The following data is based on the product molecular weight 649.08.

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.

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

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.54 mL	7.70 mL	15.41 mL
5 mM	0.31 mL	1.54 mL	3.08 mL
10 mM	0.15 mL	0.77 mL	1.54 mL
50 mM	0.03 mL	0.15 mL	0.31 mL

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References for RS 102221 hydrochloride

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

Bonhaus Absorption and brain penetration of a high affinity, highly selective 5-HT_2C receptor antagonist, RS-102221. Ann.N.Y.Acad.Sci. 1998 PMID: 9928284
Weinhardt Some benzenesulphonamido-substituted valerophenones that are selective antagonists for the 5-HT_2C receptor. Bioorg.Med.Chem.Lett.
Bonhaus RS-102221: a novel high affinity and selective 5-HT_2C receptor antagonist. Neuropharmacology 1997 PMID: 9225287