A dual orexin receptor antagonist
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SB-649868

Item No. 29477

Technical Information
Formal Name
N-[[(2S)-1-[[5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-4-benzofurancarboxamide
CAS Number
380899-24-1
Synonyms
  • GSK 649868
Molecular Formula
C26H24FN3O3S
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 15mg/mLDMF:PBS (pH 7.2) (1:20): 0.04mg/mLDMSO: 10mg/mLEthanol: 0.3mg/mL
λmax
210, 268 nm
SMILES
O=C(C1=C(C2=CC=C(F)C=C2)SC(C)=N1)N3CCCC[C@H]3CNC(C4=C(C=CO5)C5=CC=C4)=O
InChi Code
InChI=1S/C26H24FN3O3S/c1-16-29-23(24(34-16)17-8-10-18(27)11-9-17)26(32)30-13-3-2-5-19(30)15-28-25(31)21-6-4-7-22-20(21)12-14-33-22/h4,6-12,14,19H,2-3,5,13,15H2,1H3,(H,28,31)/t19-/m0/s1
InChi Key
ZJXIUGNEAIHSBI-IBGZPJMESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    SB-649868 is a dual antagonist of orexin 1 receptor (OX1R) and OX2R (Kis = 0.31 and 0.39 nM, respectively).1 In vivo, SB-649868 (3 and 10 mg/kg) decreases wakefulness and latency to fall asleep in rats.2 It also reduces binge eating of highly palatable food in a female rat model of stress-induced binge eating.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Winrow, C.J., and Renger, J.J. Discovery and development of orexin receptor antagonists as therapeutics for insomnia. Br. J. Pharmacol. 171(2), 283-293 (2014).

    2. Piccoli, L., Micioni Di Bonaventura, M.V., Cifani, C., et al. Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats. Neuropsychopharmacology 37(9), 1999-2011 (2012).