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.
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Store at +4°C
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For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Sold for research purposes under agreement from GlaxoSmithKline.
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