中文名称: | GS143 | ||||
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英文名称: | GS143 | ||||
别名: | 4-(3-苄基-4-((5-(2-氟苯基)呋喃-2-基)亚甲基)-5-氧代-4,5-二氢-1H-吡唑-1-基)苯甲酸 4-(3-Benzyl-4-{[5-(2-fluorophenyl)furan-2-yl]methylidene}-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid | ||||
CAS No: | 916232-21-8 | 分子式: | C28H19FN2O4 | 分子量: | 466.46 |
CAS No: | 916232-21-8 | ||||
分子式: | C28H19FN2O4 | ||||
分子量: | 466.46 |
基本信息
产品编号: |
G10623 |
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产品名称: |
GS143 |
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CAS: |
916232-21-8 |
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: |
466.46 |
-20℃ |
1个月 |
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化学名: |
4-(3-Benzyl-4-{[5-(2-fluorophenyl)furan-2-yl]methylidene}-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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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 |
2.1438mL |
10.7190mL |
21.4381mL |
5mM |
0.4288mL |
2.1438mL |
4.2876mL |
10mM |
0.2144mL |
1.0719mL |
2.1438mL |
生物活性
产品描述 |
一种选择性的IκBα泛素化抑制剂,对于SCFβTrCP1介导的IκBα泛素化作用的IC50为5.2μM。GS143抑制靶基因的NF-κB活化和转录,并且不抑制蛋白酶体的活性,并具有抗哮喘作用。 |
靶点 |
IC50:5.2μM(SCFβTrCP1-mediated IκBα ubiquitylation) |
体外研究 |
GS143 (10μM or 20μM) inhibits antigen-induced differentiation of Th2 cells but not of Th1 cells in vitro.The IL-4 production in Th2-polarizing condition is markedly suppressed by GS143 in a dose-dependent manner.GS143 suppresses the transcription of TNFα-induced NF-κB with a mean IC50 value of 10.5μM.GS143 also inhibits TNFαinduced expression of ICAM-1 in HT-29 colon cancer cells with an IC50 value of 6.1μM.The production levels of TNFα and IL-1β in LPS-activated THP-1 cells are inhibited with IC50 values of 5.3μM and 2.1μM,respectively.GS143 does not inhibit p53 and β-catenin. |
体内研究 |
GS143 (16-32μg/body;intranasal administration;once;BALB/c mice) treatment suppresses antigen-induced NF-κB activation in the lung of sensitized mice.GS143 treatment also inhibits antigen-induced eosinophil and lymphocyte Mrecruitment into the airways and the expression of Th2 cytokines and eotaxin in the airways. |
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 )