SB271046
目录号 : GC14550
An orally-available 5-HT6 antagonist
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 | |
| 化学名 | 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 | ||
| 分子式 | C20H22ClN3O3S2 | 分子量 | 451.99 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet