Biological Activity
5-HT2C/2B receptor antagonist (pKi values are 7.0, 8.1 and 9.1 at 5-HT2A, 2B and 2C receptors respectively). Displays inverse agonism in a 5-HT-stimulated PI hydrolysis model of 5-HT2C receptor function. Orally active in vivo.
Licensing Information
Sold under license
Compound Libraries
SB 228357 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 431.39 |
| Formula | C22H17F4N3O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 181629-93-6 |
| PubChem ID | 443390 |
| InChI Key | RRJLJKRFFRZRAF-UHFFFAOYSA-N |
| Smiles | COC1=C(C=C2N(CCC2=C1)C(=O)NC1=CC(F)=CC(=C1)C1=CC=CN=C1)C(F)(F)F |
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 | |||
| DMSO | 43.14 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 431.39. 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 | 2.32 mL | 11.59 mL | 23.18 mL |
| 5 mM | 0.46 mL | 2.32 mL | 4.64 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.32 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bromidge et al (2000) Biarylcarbamoylindolines are novel and selective 5-HT2C receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic ag J.Med.Chem. 43 1123 PMID: 10737744
Reavill et al (1999) Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br.J.Pharmacol. 126 572 PMID: 10188965
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