SB 223412
Biological Activity
Potent and selective non-peptide NK3 receptor antagonist (Ki values are 1, 144 and >100000 nM for human NK3, NK2 and NK1 receptors respectively). Selective over a panel of >60 receptors, enzymes and ion channels at concentrations of 1 or 10 μM. Inhibits NKB-induced Ca2+ mobilization in vitro (IC50 = 16.6 nM) and inhibits NK3-agonist-induced behavioral responses in vivo. Orally active and brain penetrant.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Technical Data
| M. Wt | 382.45 |
| Formula | C25H22N2O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 174636-32-9 |
| PubChem ID | 5311424 |
| InChI Key | BIAVGWDGIJKWRM-FQEVSTJZSA-N |
| Smiles | OC1=C(C(N[C@@H](CC)C2=CC=CC=C2)=O)C3=CC=CC=C3N=C1C4=CC=CC=C4 |
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 | 38.24 | 100 | |
| ethanol | 38.24 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 382.45. 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 | 2.61 mL | 13.07 mL | 26.15 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.23 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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References
References are publications that support the products' biological activity.
Sarau et al (1997) Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist. J.Pharmacol.Ther.Exp. 281 1303 PMID: 9190866
Sarau et al (2001) Molecular and pharmacological characterization of the murine tachykinin NK3 receptor. Eur.J.Pharmacol. 413 143 PMID: 11226387
de la Flor and Dawson (2009) Augmentation of antipsychotic-induced neurochemical changes by the NK3 receptor antagonist talnetant (SB-223412). Neuropharmacol. 56 342 PMID: 18822303
If you know of a relevant reference for SB 223412, please let us know.
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Keywords: SB223412 Potent selective non-peptide NK3 antagonists Brain penetrant Tachykinin Receptors Neurokinin orally active NK3 Receptor
Citations for SB 223412
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