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> G Protein-Coupled Receptor Ligands>Orexin Receptors>SB674042

Orexin Receptors

SB674042 View larger

SB674042

AOB3582

CAS No: 483313-22-0

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

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QuantitymgUnit Price ($/mg or $/Unit)Final Price
15 $16.15 Total: $80.75
110 $13.68 Total: $136.80
125 $11.59 Total: $289.75
150 $9.88 Total: $494.00
1100 $8.55 Total: $855.00

Data sheet

Molecular FormulaC24H21FN4O2S
Molecular Weight448.51
CAS Numbers483313-22-0
Storage Condition+4°C
SolubilitySoluble to 100 mM in DMSO and to 100 mM in ethanol
SMILES CodeFC1=C(C2=C(C(N3[C@H](CC4=NN=C(C5=CC=CC=C5)O4)CCC3)=O)N=C(C)S2)C=CC=C1
References1) 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.

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-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA). Molecular Pharmacology (2010), 78(1), 81-93.

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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

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