Cat. No. 4672
Chemical Name: 3-Hydroxy-2-phenyl-N-[(1S)-1-phenyl
Biological ActivityPotent 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 InformationSold for research purposes under agreement from GlaxoSmithKline.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
Sarau et al (2001) Molecular and pharmacological characterization of the murine tachykinin NK3 receptor. Eur.J.Pharmacol. 413 143. PMID: 11226387.
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.
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Keywords: SB 223412, supplier, SB223412, Potent, selective, non-peptide, NK3, antagonists, Brain, penetrant, Tachykinin, Receptors, Neurokinin, orally, active, Tocris Bioscience, NK3 Receptor Antagonist products
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July 8 - 12, 2017