中文名称: | 匹莫齐特 | ||||
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英文名称: | Pimozide | ||||
别名: | 哌莫齐特 3-[1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl]-1H-benzimidazol-2-one | ||||
CAS No: | 2062-78-4 | 分子式: | C28H29F2N3O | 分子量: | 461.55 |
CAS No: | 2062-78-4 | ||||
分子式: | C28H29F2N3O | ||||
分子量: | 461.55 | ||||
MDL: | MFCD00055081 | EINEC: | 218-171-7 | ||
EINEC: | 218-171-7 |
基本信息
产品编号: |
P10976 |
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产品名称: |
Pimozide |
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CAS: |
2062-78-4 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
461.55 |
-20℃ |
1个月 |
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化学名: |
PIMOZIDE1-{1-[4,4-BIS-(4-FLUORO-PHENYL)-BUTYL]-PIPERIDIN-4-YL}-1,3-DIHYDRO-BENZOIMIDAZOL-2-ONE |
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Solubility (25°C): |
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体外:
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DMSO |
92mg/mL warmed with 50ºC water bath (199.32mM) |
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Ethanol |
9mg/mL warmed with 50ºC water bath (19.49mM) |
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Water |
Insoluble |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.1666mL |
10.8331mL |
21.6661mL |
5mM |
0.4333mL |
2.1666mL |
4.3332mL |
10mM |
0.2167mL |
1.0833mL |
2.1666mL |
50mM |
0.0433mL |
0.2167mL |
0.4333mL |
生物活性
产品描述 |
dopamine receptor 的拮抗剂,对 dopamine D2,D3 和 D1 受体的 Ki 值分别为 1.4nM,2.5nM 和 588nM,同时对 α1-adrenoceptor 也有较高亲和性,Ki 值为 39nM;Pimozide 也是 STAT3 和 STAT5 的抑制剂。 |
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靶点 |
Dopamine Receptor |
Adrenergic Receptor |
STAT |
体外研究 |
Pimozide is a dopamine receptor antagonist,with Kis of 1.4nM,2.5nM and 588nM for dopamine D2,D3 and D1 receptors,respectively;also has affinity at α1-adrenoceptor and 5-HT1A,with Kis of 39nM and 310nM,respectively.Pimozide acts as an inhibitor of STAT3.Pimozide (0-15μM) shows inhibitory of the proliferation of U2OS cells,with IC50 value at 24,48,and 72h of 22.16±2.54,17.49±1.14 and 13.78±0.34μM,respectively. Pimozide (10μM) inhibits the colony-and sphere-forming abilities of osteosarcoma cells.Pimozide (15μM) induces G0/G1 phase cell cycle arrest,suppresses the extracellular signalregulated kinase (Erk) signaling to inhibit cell viability,and produces ROS generation through inhibiting antioxidant enzyme gene catalase expression in osteosarcoma cells.Pimozide acts as an inhibitor of STAT5.Pimozide reduces the expression of endogenous STAT5 target genes,and decreases STAT5 tyrosine phosphorylation. |
推荐实验方法(仅供参考)
细胞实验: |
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Cell proliferation is assessed by WST-8 colorimetric assay. Human osteosarcoma cells are plated in 96-well plates with 2,500 cells per well and exposed to the treatment of different concentrations of pimozide for various time intervals (24h,48h,and 72h).The WST-8 solution is added to each well after indicated time. After incubated at 37℃ for another 4 hours,the absorbance ismeasured at 450nm using a multi-well plate reader. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )