SB-674042

Cas No.:	483313-22-0
Chemical Name:	SB-674042
Synonyms:	SB-674042;[5-(2-fluorophenyl)-2-methyl-1,3-thiazol-4-yl]-[(2S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]pyrrolidin-1-yl]methanone;SB 674042;[3H]SB-674042;[5-(2-fluorophenyl)-2-methyl-thiazol-4-yl]-[(2S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]pyrrolidin-1-yl]methanone;CHEMBL2110363;CS-0934;HY-10898;SureCN1586957;(2S)- 1-[[5-(2-Fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]-pyrrolidine (9CI);(S)-1-[5-[2-Fluorophenyl]-2-methylthiazol-4-yl]-1-[2-[[5-phenyl-[1,3,4]oxadiazol-2-yl]methyl]pyrrolidin-1-yl]methanone
SMILES:	C1C=CC(C2=NN=C(C[C@@H]3CCCN3C(C3N=C(C)SC=3C3=CC=CC=C3F)=O)O2)=CC=1
Formula:	C24H21FN4O2S
M.Wt:	448.512547254562
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM); exhibits 100-fold selectivity for OX1 over OX2 receptors. SB-674042 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.
Target:	OX1 receptor
References:	[1]. Heifetz, Alexander; Morris, G. Benjamin; Biggin, Philip C. et al. Study of Human Orexin-1 and -2 G-Protein-Coupled Receptors with Novel and Published Antagonists by Modeling, Molecular Dynamics Simulations, and Site-Directed Mutagenesis. Biochemistry (201 [2]. Malherbe, Pari; Roche, Olivier; Marcuz, Anne et al. Mapping the binding pocket of dual antagonist Almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-me [3]. Malherbe, Pari; Borroni, Edilio; Pinard, Emmanuel et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Molecular P [4]. Ellis, James; Pediani, John D.; Canals, Meritxell et al. Orexin-1 Receptor-Cannabinoid CB1 Receptor Heterodimerization Results in Both Ligand-dependent and -independent Coordinated Alterations of Receptor Localization and Function. Journal of Biological C [5]. Langmead, Christopher J.; Jerman, Jeffrey C.; Brough, Stephen J. et al. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. British Journal of Pharmacology (2004), 141(2), 340-346.