A 5-HT6 receptor antagonist
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SB-399885 (hydrochloride)

Item No. 32817

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3,5-dichloro-2-methoxyphenyl)-4-methoxy-3-(1-piperazinyl)-benzenesulfonamide, monohydrochloride
CAS Number
402713-81-9
Molecular Formula
C18H21Cl2N3O4S • HCl
Formula Weight
482.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
O=S(NC1=C(OC)C(Cl)=CC(Cl)=C1)(C2=CC=C(C(N3CCNCC3)=C2)OC)=O.Cl
InChi Code
InChI=1S/C18H21Cl2N3O4S.ClH/c1-26-17-4-3-13(11-16(17)23-7-5-21-6-8-23)28(24,25)22-15-10-12(19)9-14(20)18(15)27-2;/h3-4,9-11,21-22H,5-8H2,1-2H3;1H
InChi Key
RNKCEBCFUSXSQE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $143

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    10 mg

    $255

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    25 mg

    $561

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    50 mg

    $1,053

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    Product Description

    SB-399885 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.72 nM).1 It is greater than 200-fold selective for 5-HT6 receptors over a panel of receptors, ion channels, and enzymes at 10 µM. SB-399885 inhibits 5-HT-induced cAMP accumulation in HeLa cells expressing recombinant human 5-HT6 receptors (pA2 = 7.85). In vivo, SB-399885 increases the seizure threshold in a rat model of seizures induced by maximal electroshock (MES). It reduces escape latency in the Morris water maze in aged rats and reverses scopolamine-induced impairments in the novel object recognition task in adult rats when administered at a dose of 10 mg/kg. SB-399885 (10 mg/kg) decreases immobility time in the forced swim and tail suspension tests in mice.2 It also increases drinking in the Vogel punished drinking task, indicating anxiolytic-like activity, in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hirst, W.D., Stean, T.O., Rogers, D.C., et al. SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. Eur. J. Pharmacol. 553(1-3), 109-119 (2006).

    2. Wesołowska, A., and Nikiforuk, A. Effects of the brain-penetrant and selective 5-HT6 receptor antagonist SB-399885 in animal models of anxiety and depression. Neuropharmacology 52(5), 1274-1283 (2007).