SB 674042

Cat. No. 4673

SB 674042  [483313-22-0]

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Chemical Name: [5-(2-Fluorophenyl)-2-methyl-4-thiazolyl][2(S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl-1-pyrrolidinyl]methanone

Biological Activity

Potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM). Exhibits 100-fold selectivity for OX1 over OX2 receptors. Has no effect at serotonergic, dopaminergic, adrenergic or purinergic receptors. Inhibits orexin 1-induced Ca2+ mobilization in CHO-DG44 cells stably transfected with the OX1 receptor.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data

Soluble to 100 mM in DMSO and to 100 mM in ethanol
Store at +4°C

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 / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Ellis et al (2006) Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. Biol.Chem. 281 38812. PMID: 17015451.

Langmead et al (2004) Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br.J.Pharmacol. 141 340. PMID: 14691055.

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Keywords: SB 674042, supplier, Potent, selective, non, peptide, OX1, receptors, antagonists, orexin1, orexin-1, SB674042, Tocris Bioscience, OX1 Receptor Antagonist products

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