CAS 209481-20-9|SB271046

Introduction:Basic information about CAS 209481-20-9|SB271046, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameSB271046
CAS Number209481-20-9Molecular Weight488.45100
Density1.400Boiling Point664.3ºC at 760 mmHg
Molecular FormulaC20H23Cl2N3O3S2Melting Point240-241℃ (DEC.)
MSDS/Flash Point355.5ºC

Names

NameSB 271046 hydrochloride
SynonymMore Synonyms

SB271046 BiologicalActivity

DescriptionSB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity[1].
Related CatalogResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor
Target

5-HT6 Receptor:8.92-9.09 (pKi)

In VitroIn functional studies on human 5-HT6 receptors SB 271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71[1].
In VivoSB 271046 produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg/kg p.o. and maximum effect at 4 h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB 271046 (EC50 of 0.16 μM) and brain concentrations of 0.01-0.04 μM at Cmax[1].
References

[1]. C Routledge, et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000 Aug;130(7):1606-12.

Chemical & Physical Properties

Density1.400
Boiling Point664.3ºC at 760 mmHg
Melting Point240-241℃ (DEC.)
Molecular FormulaC20H23Cl2N3O3S2
Molecular Weight488.45100
Flash Point355.5ºC
Exact Mass487.05600
PSA107.29000
LogP6.43170
InChIKeyLOCQRDBFWSXQQI-UHFFFAOYSA-N
SMILESCOc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCNCC1
Storage conditionDesiccate at RT

Synonyms

5-Chloro-N-[4-methoxy-3-(piperazin-1-yl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamide hydrochloride (1:1)
Benzo[b]thiophene-2-sulfonamide, 5-chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-, hydrochloride (1:1)
5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-1-benzothiophene-2-sulfonamide hydrochloride (1:1)
Benzo[b]thiophene-2-sulfonamide (5-chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl
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