A potent and selective orexin 1 receptor antagonist
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SB-674042

Item No. 21270

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[5-(2-fluorophenyl)-2-methyl-4-thiazolyl][(2S)-2-[(5-phenyl-1,3,4-oxadiazol-2-yl)methyl]-1-pyrrolidinyl]-methanone
CAS Number
483313-22-0
Molecular Formula
C24H21FN4O2S
Formula Weight
448.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/ml
λmax
252 nm
SMILES
O=C(C1=C(C2=CC=CC=C2F)SC(C)=N1)N3[C@H](CC4=NN=C(C5=CC=CC=C5)O4)CCC3
InChi Code
InChI=1S/C24H21FN4O2S/c1-15-26-21(22(32-15)18-11-5-6-12-19(18)25)24(30)29-13-7-10-17(29)14-20-27-28-23(31-20)16-8-3-2-4-9-16/h2-6,8-9,11-12,17H,7,10,13-14H2,1H3/t17-/m0/s1
InChi Key
HYBZWVLPALMACV-KRWDZBQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $38

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    5 mg

    $129

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    10 mg

    $238

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    25 mg

    $543

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    Product Description

    SB-674042 is a potent and selective non-peptide orexin 1 receptor (OX1R) antagonist (Kd = 5.03 and 3.76 nM in whole cell binding and membrane-based assays, respectively).1 In calcium mobilization studies, it was >100-fold selective for OX1 over OX2 and did not show significant affinity for serotonergic, dopaminergic, adrenergic, or purinergic receptors at concentrations up to 10 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Langmead, C.J., Jerman, J.C., Brough, S.J., et al. Characterisation of the binding of 3H-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br. J. Pharmacol. 141(2), 340-346 (2004).

    2. Ellis, J., Pediani, J.D., Canals, M., et al. Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. The Journal of Biological Chemisty 281(50), 38812-38824 (2006).