SB 223412

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Cat.No. 4672 - SB 223412 | CAS No. 174636-32-9
Description: Potent, selective non-peptide NK3 antagonist. Brain penetrant
Chemical Name: 3-Hydroxy-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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.

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

Safety Datasheet

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


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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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