A potent orexin 1 receptor antagonist
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SB-408124

Item No. 22961

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(6,8-difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]-urea
CAS Number
288150-92-5
Molecular Formula
C19H18F2N4O
Formula Weight
356.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 20 mg/mlEthanol: 0.5 mg/ml
λmax
227, 265, 315 nm
SMILES
FC1=CC(F)=CC2=C1N=C(C)C=C2NC(NC3=CC=C(N(C)C)C=C3)=O
InChi Code
InChI=1S/C19H18F2N4O/c1-11-8-17(15-9-12(20)10-16(21)18(15)22-11)24-19(26)23-13-4-6-14(7-5-13)25(2)3/h4-10H,1-3H3,(H2,22,23,24,26)
InChi Key
JTARFZSNUAGHRB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $158

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    25 mg

    $349

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    50 mg

    $523

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    Product Description

    SB-408124 is a potent antagonist of orexin 1 receptors (OX1Rs) with a Ki value of 26.9 nM in a calcium mobilization assay using CHO cells that stably express human OX1R.1 It is selective for OX1R over OX2R, with Kd values of 21.7 and 1,704 nM, respectively, in a radioligand binding assay. In vivo co-perfusion of SB-408124 with human OX1R in the rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations and reduces cocaine-seeking behavior in rats.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. Wang, B., You, Z.B., and Wise, R.A. Reinstatement of cocaine seeking by hypocretin (orexin) in the ventral tegmental area: Independence from the local corticotropin-releasing factor network. Biol. Psychiatry 65(10), 857-862 (2009).