SB 228357

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Cat.No. 1375 - SB 228357 | C22H17F4N3O2 | CAS No. 181629-93-6
Description: 5-HT2C/2B antagonist/inverse agonist
Chemical Name: N-[3-Fluoro-5-(3-pyrindyl)phenyl]-2,3-dihydro-5-methoxy-6-(trifluoromethyl)-1H-indole-1-carboxamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

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

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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

Safety Datasheet

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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Keywords: SB 228357, supplier, 5-HT2C, 5-HT2B, antagonists, inverse, agonists, Serotonin, Receptors, SB228357, 5-HT2C, Receptors, 5-HT2B, Receptors, 5-HT2C, Receptors, Tocris Bioscience

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