SB-674042, inhibitor

SB-674042

Cat. Num. AAA5755509

• Purity: 98.00%
• Synonyms: SB-674042; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 32mg/mL (71.35mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C24H21FN4O2S
• SMILES: FC1=C(C2=C(C(N3[C@H](CC4=NN=C(C5=CC=CC=C5)O4)CCC3)=O)N=C(C)S2)C=CC=C1
• CAS Number: 483313-22-0
• Target & IC50: Others
• In Vitro: OX1 receptor SB-674042 has no effect on serotonergic, dopaminergic, adrenergic, or purinergic receptors. Inhibits orexin 1-induced Ca2+ mobilization in CHO-DG44 cells stably transfected with the OX1 receptor.
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for SB-674042, inhibitor

SB-674042 is an effective and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76nM). It exhibits 100-fold selectivity for OX1 over OX2 receptors.

References

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 (2012), 51(15), 3178-3197.
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 (2012), 51(15), 3178-3197.
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-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA). Molecular Pharmacology (2010), 78(1), 81-93.
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-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA). Molecular Pharmacology (2010), 78(1), 81-93.
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 Pharmacology (2009), 76(3), 618-631.
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 Pharmacology (2009), 76(3), 618-631.
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 Chemistry (2006), 281(50), 38812-38824.
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 Chemistry (2006), 281(50), 38812-38824.
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.
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.