SB271046 |
Catalog No.GC14550
One-Click Copy Product Info
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SB271046은 pKi가 8.92-9.09인 강력하고 선택적이며 경구 활성인 5-HT6 수용체 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 209481-20-9
Sample solution is provided at 25 µL, 10mM.
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SB-271046 is a selective and orally active 5-HT6 receptor antagonist.
5-HT6 belongs to GPCR which stimulates adenylate cyclase via Gs, which cloned from rat striatum.
SB-271046 substituted [125I]-SB-258585 and [3H]-LSD from human 5-HT6 receptors which recombinantly expressed in HeLa cells in vitro (pKi 8.92 and 9.09 respectively). SB-271046 also transfered [125I]-SB-258585 from human caudate putamen and rat and pig striatum membranes (pKi 8.81, 9.02 and 8.55 respectively). By 5-HT alone or after increasing concentrations of SB-271046 (10, 30, 100 and 300 nM) stimulates adenylyl cyclase activity in HeLa cells stably expressing human 5-HT6 receptors. [1]
The affinities of SB-271046 in human (pKi 8.81), pig (pKi 8.55) and rat (pKi 9.02) were similar suggesting a lack of species differences in 5-HT6 receptor for this given ligand. SB-271046 has greater than 200 fold selectivity over 69 other receptor, enzyme and binding sites, containing all other 5-HT receptor subtypes tested. SB-271046 did not alter basal levels of 5-HT, DA and NA in either brain region. In contrast, administration of SB-271046 (10mg.kg-1s.c.) produced an important and tetrodotoxin-dependent acceleration in extracellular levels of both glutamate and aspartate within the frontal cortex, reaching maximum values of 375.482.3 and 215.362.1% of preinjection values, respectively. [2]
References:
1. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000 Aug;130(7):1606-12.
2. In vivo effects of the 5-HT(6) antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, dopamine, 5-HT, glutamate and aspartate. Br J Pharmacol. 2000 May;130(1):23-6.
| Cas No. | 209481-20-9 | SDF | |
| Chemical Name | 5-chloro-N-(4-methoxy-3-piperazin-1-ylphenyl)-3-methyl-1-benzothiophene-2-sulfonamide;hydrochloride | ||
| Canonical SMILES | CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC(=C(C=C3)OC)N4CCNCC4.Cl | ||
| Formula | C20H22ClN3O3S2 | M.Wt | 451.99 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2124 mL | 11.0622 mL | 22.1244 mL |
| 5 mM | 442.5 μL | 2.2124 mL | 4.4249 mL |
| 10 mM | 221.2 μL | 1.1062 mL | 2.2124 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)