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SB-399885 hydrochloride
CAS No. 402713-81-9
SB-399885 hydrochloride( SB399885 )
Catalog No. M14379 CAS No. 402713-81-9
SB-399885 is a potent, selective, brain penetrant 5-HT6 receptor antagonist.
SB-399885 is a potent, selective, brain penetrant 5-HT6 receptor antagonist.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
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Biological Information
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Product NameSB-399885 hydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionSB-399885 is a potent, selective, brain penetrant 5-HT6 receptor antagonist.
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DescriptionSB-399885 is a potent, selective, brain penetrant 5-HT6 receptor antagonist with pKi of 9.11 and 9.02 for human recombinant and native 5-HT6 receptors; SB-399885 is a potent competitive antagonist (pA(2)=7.85), displays over 200-fold selectivity over other receptors; significantly increases extracellular acetylcholine levels in rat medial prefrontal cortex, exhibits cognitive enhancing properties in recognition models; also is an inhibitor of HCV entry in liver-derived cell lines as well as primary hepatocytes, modulates localization of the coreceptor tight junction protein claudin-1 (CLDN1) in a 5-HT6-independent manner, induces intracellular accumulation of CLDN1.
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In Vitro——
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In VivoCompare with the control vehicle SB-399885 hydrochloride 10 mg/kg significantly increases wakefulness (W) (F(3,15)=3.32, P<0.05) while slow wave sleep (SWS), rapid-eye-movement sleep (REMS) and the number of REM periods are reduced (F(3,15)=4.0, P<0.01; F(3,15)=3.14, P<0.05 and F(3,15)=2.62, P<0.05, respectively). Analysis of sleep variables in 2-h blocks shows that SB-399885 hydrochloride 10 mg/kg increases W (F(3,15)=5.48, P<0.01) and reduces SWS (F(3,15)=5.42, P<0.01) and REMS (F(3,15)= 4.05, P<0.01) during the first 2-h period. SB-399885 hydrochloride 5 and 10 mg/kg augment light sleep over the first (F(3,15)=3.46,P<0.01 and F(3,15)= 3.65, P<0.01, respectively) and the second (F(3,15)=3.23, P<0.05 and F(3,15)=3.08, P<0.05, respectively) 2-h recording periods. SB-399885 hydrochloride 10 mg/kg significantly increases REMS latency (F(3,15)=3.60, P<0.01) and reduces the number of REM periods during the first 2-h of recording (F(3,15)=3.88, P<0.01).
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SynonymsSB399885
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PathwayEndocrinology/Hormones
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Target5-HT Receptor
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Recptor5-HT Receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number402713-81-9
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Formula Weight482.801
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Molecular FormulaC18H22Cl3N3O4S
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Purity>98% (HPLC)
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SolubilityDMSO : 125 mg/mL 258.90 mM
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SMILESCOC1=C(C=C(C=C1)S(=O)(=O)NC2=C(C(=CC(=C2)Cl)Cl)OC)N3CCNCC3.Cl
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Chemical NameN-(3,5-dichloro-2-methoxyphenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide hydrochloride
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Weso?owska A, et al. Eur J Pharmacol. 2008 Mar 17;582(1-3):88-93.
2. Riva L, et al. J Virol. 2018 Apr 27;92(10). pii: e01982-17.
3. Hirst WD, et al. Eur J Pharmacol. 2006 Dec 28;553(1-3):109-19.
4. Weso?owska A, et al. Neuropharmacology. 2007 Apr;52(5):1274-83.
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