SB 223412

Key Product Details

Product Description

SB 223412 is a potent and selective non-peptide NK₃ receptor antagonist (K_i 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.

Product Specifications for SB 223412

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for SB 223412

The following data is based on the product molecular weight 382.45.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

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

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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

Calculators

Background References

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

• Sarau Molecular and pharmacological characterization of the murine tachykinin NK₃ receptor. Eur.J.Pharmacol. 2001 PMID: 11226387
• de la Flor and Dawson Augmentation of antipsychotic-induced neurochemical changes by the NK₃ receptor antagonist talnetant (SB-223412). Neuropharmacol. 2009 PMID: 18822303
• Sarau 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. 1997 PMID: 9190866

Product Documents for SB 223412