SB 271046 HCl (SB-271046A)

Alias: SB-271046; SB 271046; SB271046; SB-271046 HCl; SB-271046 hydrochloride
Cat No.:V0980 Purity: ≥98%
SB271046 HCl (SB 271046; SB-271046), the hydrochloride salt of SB 271046, is a novel, potent, selective and orally bioactive 5-HT6 receptor antagonist with potential anticonvulsant activity.
SB 271046 HCl (SB-271046A) Chemical Structure CAS No.: 209481-24-3
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Other Forms of SB 271046 HCl (SB-271046A):

  • SB-271046
  • SB 271046 (SB-271046A)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SB271046 HCl (SB 271046; SB-271046), the hydrochloride salt of SB 271046, is a novel, potent, selective and orally bioactive 5-HT6 receptor antagonist with potential anticonvulsant activity. It has 200 times more selectivity than other 5-HT receptor subtypes and inhibits 5-HT6 with a pKi of 8.9.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT6 Receptor ( pKi = 8.92-9.02 ); 5-HT1D Receptor ( pKi = 6.55 ); 5-HT1A Receptor ( pKi = 6.35 ); 5-HT1B Receptor ( pKi = 6.05 ); 5-HT1F Receptor ( pKi = 5.95 );
5-HT2A Receptor ( pKi = 5.62 ); 5-HT2B Receptor ( pKi = 5.41 ); 5-HT7 Receptor ( pKi = 5.39 ); 5-HT4 ( pKi = 5.27 ); 5-HT1E ( pKi < 4.99 );
Human 5-HT2C Receptor ( pKi = 5.73 )
ln Vitro

In vitro activity: SB 271046 Hydrochloride (SB 271046A) exhibits pKi values of 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27, and less than 4.99 at 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E, independently. SB-271046 hydrochloride competitively opposes 5-HT-induced adenylyl cyclase activity stimulation with a pA2 of 8.71[1].

ln Vivo
SB 271046 Hydrochloride (10 mg/kg; p.o.) generates a broad dose-dependent increase in seizure threshold in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of approximately 0.1 mg/kg p.o. and a maximum effect occurring 4 hours after the dose[1].
Enzyme Assay
SB271046 Hcl is an effective, pKi of 8.9, selective, and oral 5-HT6 receptor antagonist. IC50 Value: 8.9(pKi). A sulfonamidal benzothiophene derivative, SB 271046 hydrochloride has been demonstrated to function as a selective 5-HT6 antagonist, with pKi values of 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27, and < 4.99 for 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E, respectively. It is also > 200-fold selective over 55 other receptors, enzymes, and ion channels.
Animal Protocol
Dissolved in 1% methyl cellulose in water; 30 mg/kg; Oral gavage
Male Sprague Dawley rats
References

[1]. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000;130(7):1606-1612.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H23CL2N3O3S2
Molecular Weight
488.45
Exact Mass
487.06
Elemental Analysis
C, 49.18; H, 4.75; Cl, 14.52; N, 8.60; O, 9.83; S, 13.13
CAS #
209481-24-3
Appearance
Solid powder
SMILES
CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC(=C(C=C3)OC)N4CCNCC4.Cl
InChi Key
RMXZRJYGJMSDQK-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H22ClN3O3S2.ClH/c1-13-16-11-14(21)3-6-19(16)28-20(13)29(25,26)23-15-4-5-18(27-2)17(12-15)24-9-7-22-8-10-24;/h3-6,11-12,22-23H,7-10H2,1-2H3;1H
Chemical Name
5-chloro-N-(4-methoxy-3-piperazin-1-ylphenyl)-3-methyl-1-benzothiophene-2-sulfonamide;hydrochloride
Synonyms
SB-271046; SB 271046; SB271046; SB-271046 HCl; SB-271046 hydrochloride
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 40~50 mg/mL (81.9~102.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
1% methylcellulose: ~30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0473 mL 10.2365 mL 20.4729 mL
5 mM 0.4095 mL 2.0473 mL 4.0946 mL
10 mM 0.2047 mL 1.0236 mL 2.0473 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • SB 271046 HCl

    (a) Stimulation of adenylyl cyclase activity in HeLa cells stably expressing human 5-HT6 receptors by 5-HT alone and in the presence of increasing concentrations of SB-271046.Br J Pharmacol.2000 Aug;130(7):1606-12.
  • SB 271046 HCl
    Time course profile of anticonvulsant activity in the MEST test and blood concentration of SB-271046 in rats.Br J Pharmacol.2000 Aug;130(7):1606-12.
  • SB 271046 HCl
    Relationship between SB-271046 blood concentration and seizure threshold.Br J Pharmacol.2000 Aug;130(7):1606-12.
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