中文名称: | 瑞沙托维 | ||||
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英文名称: | Resatorvid | ||||
别名: | 瑞沙托维 TAK-242; CLI-095 | ||||
CAS No: | 243984-11-4 | 分子式: | C15H17ClFNO4S | 分子量: | 361.82 |
CAS No: | 243984-11-4 | ||||
分子式: | C15H17ClFNO4S | ||||
分子量: | 361.82 |
基本信息
产品编号: |
R10252 |
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产品名称: |
Resatorvid |
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CAS: |
243984-11-4 |
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: |
361.82 |
-20℃ |
1个月 |
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化学名: |
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Solubility (25°C): |
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体外:
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DMSO |
72mg/mL (198.99mM) |
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Ethanol |
72mg/mL (198.99mM) |
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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 |
2.7638mL |
13.8190mL |
27.6381mL |
5mM |
0.5528mL |
2.7638mL |
5.5276mL |
10mM |
0.2764mL |
1.3819mL |
2.7638mL |
50mM |
0.0553mL |
0.2764mL |
0.5528mL |
生物活性
产品描述 |
一种选择性的TLR4信号传导抑制剂。Resatorvid抑制NO,TNF-α和IL-6的产生,其IC50值分别为1.8nM,1.9nM,1.3nM。 |
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靶点 |
TLR4 |
IL-6 |
NO |
TNF-α |
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1.3nM |
1.8nM |
1.9nM |
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体外研究 |
Resatorvid suppresses the production of NO,TNF-α,and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33nM.Resatorvid (1-100nM;4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells.Resatorvid (1-100nM;15 minutes;PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signalregulated kinase 1/2 (Erk1/2),p38,and JNK/SAPK as well as degradation of IκBβ at a concentration of 100nM. RT-PCR |
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Cell Line: |
RAW264.7 cells |
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Concentration: |
1nM,10nM,100nM |
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Incubation Time: |
4 hours |
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Result: |
TNF-α and IL-6 mRNA expression levels were clearly suppressed at concentrations of 10 to 100nM. |
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Western Blot Analysis |
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Cell Line: |
PBMCs cells |
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Concentration: |
1nM,10nM,100nM |
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Incubation Time: |
15 minutes |
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Result: |
The phosphorylation of mitogen-activated protein kinases induced by LPS was also inhibited in a concentration-dependent manner. |
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体内研究 |
Resatorvid (TAK-242;3mg/kg;intraperitoneal injection;for 2 days;male C57BL/6 mice) pretreatment markedly and significantly reverses the LPS-induced body weight loss,TA muscle loss,and muscle strength loss.TAK-242 reverses the LPSinduced shrinkage of muscle fibres and increases the interstitial space.TAK-242 blocks systemic catabolic cytokine release and skeletal muscle proteolysis in LPS-administered mice. |
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Animal Model: |
Male C57BL/6 mice (8-12 weeks of age) treated with lipopolysaccharide (LPS). |
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Dosage: |
3mg/kg |
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Administration: |
Intraperitoneal injection;for 2 days |
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Result: |
Pretreatment of mice reduced or reversed all the detrimental effects of LPS. |
推荐实验方法(仅供参考)
细胞实验: |
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细胞系 |
原代角质形成细胞 |
浓度 |
10µM |
处理时间 |
6h |
方法 |
用紫外线照射NF-κB角质细胞,10µM resatorvid(或vehicle)处理6小时后,收集细胞。Resatorvid可显著地抑制紫外线诱导的NF-κB荧光素酶信号。 |
动物实验: |
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动物模型 |
4-5周龄的雄性ddY小鼠 |
剂量 |
1μl (at 0.001,0.03,or 0.01μg/μl) |
给药处理 |
侧脑室注射 |
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 )