A 5-HT6 receptor antagonist
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SB-742457

Item No. 22200

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(phenylsulfonyl)-8-(1-piperazinyl)-quinoline
CAS Number
607742-69-8
Synonyms
  • GSK742457
Molecular Formula
C19H19N3O2S
Formula Weight
353.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlEthanol: 0.1 mg/ml
λmax
273, 364 nm
SMILES
O=S(C(C=N1)=CC2=C1C(N3CCNCC3)=CC=C2)(C4=CC=CC=C4)=O
InChi Code
InChI=1S/C19H19N3O2S/c23-25(24,16-6-2-1-3-7-16)17-13-15-5-4-8-18(19(15)21-14-17)22-11-9-20-10-12-22/h1-8,13-14,20H,9-12H2
InChi Key
JJZFWROHYSMCMU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $186

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    10 mg

    $351

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    25 mg

    $775

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM).1,2 SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity.3 SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells.2 In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine (Item No. 14108) in rats.1 It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Upton, N., Chuang, T.T., Hunter, A.J., et al. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer’s disease. Neurotherapeutics 5(3), 458-469 (2008).

    2. Grychowska, K., Satała, G., Kos, T., et al. Novel 1H-pyrrolo[3,2-c]quinoline based 5-HT6 receptor antagonists with potential application for the treatment of cognitive disorders associated with Alzheimer’s disease. ACS Chem. Neurosci. 7(7), 972-983 (2016).

    3. Ivachtchenko, A.V., and Ivanekov, Y.A. Small molecule 5-HT6R Ligands: A comprehensive insight into their selectivity and activity. Curr. Bioactive Compounds 9(1), 64-100 (2013).

    4. Higgs, S., Cooper, A.J., and Barnes, N.M. The 5-HT₂C receptor agonist, lorcaserin, and the 5-HT6 receptor antagonist, SB-742457, promote satiety; a microstructural analysis of feeding behaviour. Psychopharmacology (Berl) 233(3), 417-424 (2016).