SB271046 |
| رقم الكتالوجGC14550 |
SB271046 هو مضاد لمستقبلات 5-HT6 فعال وانتقائي وفعال عن طريق الفم مع pKi من 8.92-9.09.
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 |
| الذوبان | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2124 mL | 11.0622 mL | 22.1244 mL |
| 5 mM | 0.4425 mL | 2.2124 mL | 4.4249 mL |
| 10 mM | 0.2212 mL | 1.1062 mL | 2.2124 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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