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Intepirdine

产品编号 T1774 CAS 607742-69-8

别名: RVT-101, SB 742457, GSK-742457

Intepirdine (GSK-742457) 是5-HT6受体拮抗剂，pKi 为9.63，用于研究阿尔茨海默病治疗的试验。

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Intepirdine, CAS 607742-69-8

规格	价格/CNY	货期
1 mg	￥ 298	现货
5 mg	￥ 690	现货
10 mg	￥ 1,120	现货
25 mg	￥ 2,230	现货
50 mg	￥ 3,570	现货
100 mg	￥ 5,660	现货
500 mg	￥ 11,300	现货
1 mL * 10 mM (in DMSO)	￥ 778	现货

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选择批次

纯度: 98.99%

纯度: 98%

纯度: 95.19%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Intepirdine (GSK-742457) is a highly selective 5-HT6 receptor antagonist, used in trials studying the treatment of Alzheimer's Disease.
靶点活性	5-HT6:9.63(pKi)
体外活性	SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects. [2] SB-742457 is a novel cognitive enhancing agent for Alzheimer's disease. SB-742457 is a potential agent added to stablize donepezil treatment in subjects with mild-to-moderate Alzheimer's disease. [1]
激酶实验	In vitro kinase activity assay: EGFR kinase: Each 100 μL enzyme reaction contained 10 μL of inhibitor in 50% Me2SO, 20 μL of substrate solution (200 mM HEPES pH 7.4, 50 mM Mg-acetate, 2.5 mg/mL poly (EY), 5 μg/mL bio-pEY) and 20 μL enzyme preparation. The enzymatic reaction is started by addition of 50 μL of a 100 μM ATP solution made in 10 mM MgCl2. Assays are carried out at room temperature for 30 min and terminated by the addition of 50 μL of stop solution (250 mM EDTA in 20 mM HEPES pH 7.4). 100 μL are transferred to a streptavidin coated microtiterplate, after an incubation time of 60 min at room temperature the plate is washed with 200 μL of wash solution (50 mM Tris, 0.05% Tween20). A 100 μL aliquot of a HRPO- labeled anti-PY antibody (PY20H Anti-Ptyr:HRP ) 250 ng/mL are added to the wells. After 60 min of incubation, the plate is washed three times with a 200 μL wash solution. The samples are then developed with a 100μL TMB Peroxidase Solution (A:B= 1:1). The reaction is stopped after 10 min. The plate is transferred to an ELISA reader and extinction is measured at OD450 nM. HER2-IC enzyme: Enzyme activity is assayed in the presence or absence of serial inhibitor dilutions performed in 50 % Me2SO. Each 100 μL reaction contains similar components as described for EGFR kinase assay with addition of 1000 μM Na3VO4. The enzymatic reaction is started by addition of 50μL of 500 μM ATP solution made in 10 mM Mg-acetate. The dilution of the enzyme is set so that incorporation of phosphate into bio-pEY is linear with respect to time and amount of enzyme. The enzyme preparation is diluted in 20 mM HEPES pH 7.4, 130 mM NaCl, 0.05% Triton X-100, 1 mM DTT and 10% glycerol. Assays are carried out at room temperature for 30 min and terminated by the addition of 50 μL of stop solution. Src kinase assays: Each 100 μL reaction contained 10 μL of inhibitor in 50 % Me2SO, 20μL of enzyme preparation, 20 μL of substrate solution supplemented with 1000 μM Na3VO4.The enzymatic reaction is started by addition of 50 μL of a 1000 μM ATP solution made in 10 mM Mg-acetate. BIRK kinase assay: 250 mM Tris pH 7.4, 10 mM DTT, 2.5 mg/mL poly(EY), 5 mg/mL bio-pEY is used as substrate solution and enzymatic reaction is started by addition of 50 μL of a 2 mM ATP solution made in 8 mM MnCl2, 20 mM Mg-acetate. VEGF2 and HGFR kinase assays: Assays are carried out at room temperature for 20 minutes and terminated by the addition of 10 μL of 5 % H3PO4. The precipitate is then trapped onto GF/B filters using a 96 well filter mate universal harvester. After extensive washing the filter plate is dried for 1 h at 50°C, sealed and incorporated radioactivity is determined by scintillation counting using a TopCount? or a Microbeta b counter?.

别名	RVT-101, SB 742457, GSK-742457
分子量	353.44
分子式	C19H19N3O2S
CAS No.	607742-69-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 2 mg/mL (5.65 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 72 mg/mL (203.7 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	2.8293 mL	14.1467 mL	28.2933 mL	70.7334 mL
Ethanol / DMSO	5 mM	0.5659 mL	2.8293 mL	5.6587 mL	14.1467 mL
DMSO	10 mM	0.2829 mL	1.4147 mL	2.8293 mL	7.0733 mL
	20 mM	0.1415 mL	0.7073 mL	1.4147 mL	3.5367 mL
	50 mM	0.0566 mL	0.2829 mL	0.5659 mL	1.4147 mL
	100 mM	0.0283 mL	0.1415 mL	0.2829 mL	0.7073 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Chuang ATT, et al. Alzheimers Dement, 2006, 2, S631–S632 (abstract). 2. Upton N, et al. Neurotherapeutics, 2008, 5(3), 458-469.

文献引用

1. Rychtyk J, Partyka A, Gdula-Argasińska J, et al. 5-HT6 receptor agonist and antagonist improve memory impairments and hippocampal BDNF signaling alterations induced by MK-801. Brain Research. 2019: 146375 2. Wesołowska A, Rychtyk J, Gdula-Argasińska J, et al Effect of 5-HT6 Receptor Ligands Combined with Haloperidol or Risperidone on Antidepressant-/Anxiolytic-Like Behavior and BDNF Regulation in Hippocampus and Prefrontal Cortex of Rats. Neuropsychiatric Disease and Treatment. 2021, 17: 2105. 4. Partyka A, Górecka K, Gdula-Argasińska J, et al.Selective 5-HT6 Receptor Ligands (Agonist and Antagonist) Show Different Effects on Antipsychotic Drug-Induced Metabolic Dysfunctions in Rats.Pharmaceuticals.2023, 16(2): 154.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Intepirdine 607742-69-8 GPCR/G Protein Neuroscience 5-HT Receptor GSK 742457 Inhibitor inhibit 5-hydroxytryptamine Receptor Serotonin Receptor SB-742457 RVT-101 RVT101 GSK742457 SB 742457 GSK-742457 RVT 101 SB742457 inhibitor

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Intepirdine

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords