Biological Activity
Potent and selective 5-HT2C antagonist (pKi = 8.7). Displays ~ 100-fold selectivity over the 5-HT2A and 5-HT2B 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
RS 102221 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 100 mM in DMSO |
Preparing Stock Solutions
The following data is based on the product molecular weight 649.08. 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 | 1.54 mL | 7.7 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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Product Datasheets
References
References are publications that support the products' biological activity.
Bonhaus et al (1997) RS-102221: a novel high affinity and selective 5-HT2C receptor antagonist. Neuropharmacology 36 621 PMID: 9225287
Bonhaus et al (1998) Absorption and brain penetration of a high affinity, highly selective 5-HT2C receptor antagonist, RS-102221. Ann.N.Y.Acad.Sci. 861 269 PMID: 9928284
Weinhardt et al (1996) Some benzenesulphonamido-substituted valerophenones that are selective antagonists for the 5-HT2C receptor. Bioorg.Med.Chem.Lett. 6 2687 PMID:
Keywords: RS 102221 hydrochloride, supplier, Selective, 5-HT2C, antagonist, Serotonin, Receptors, RS102221, hydrochloride, 5-HT2C, Receptors, 5-HT2C, Receptors, Tocris Bioscience
