483313-22-0

483313-22-0 structure

Name: SB-674042
Chemical Name: [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
CAS Number: 483313-22-0
Molecular Formula: C₂₄H₂₁FN₄O₂S
Molecular Weight: 448.51300
Catalog: Signaling Pathways GPCR/G Protein Orexin Receptor (OX Receptor)
Create Date: 2017-06-02 22:02:08
Modify Date: 2025-08-25 09:12:04
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.IC50 value: 3.76 nM (Kd)Target: OX1 receptorSB-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.

Name	[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
Synonyms	[5-(2-fluorophenyl)-2-methyl-thiazol-4-yl]-[(2S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]pyrrolidin-1-yl]methanone CS-0934 SB-674042

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.IC50 value: 3.76 nM (Kd)Target: OX1 receptorSB-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.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Orexin Receptor (OX Receptor) Research Areas >> Neurological Disease
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.

Molecular Formula	C₂₄H₂₁FN₄O₂S
Molecular Weight	448.51300
Exact Mass	448.13700
PSA	100.36000
LogP	5.09280
Storage condition	2-8℃

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
RIDADR	NONH for all modes of transport

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