中文名称: | SecinH3 一键复制产品信息 | ||||
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英文名称: | SecinH3 | ||||
别名: | N-[4-[5-(1,3-苯并二氧杂环戊烯-5-基)-3-甲氧基-1H-1,2,4-噻唑-1-基]苯基]-2-(苯基硫代)乙酰胺 N-[4-[5-(1,3-Benzodioxol-5-yl)-3-methoxy-1H-1,2,4-triazol-1-yl]phenyl]-2-(phenylthio)acetamide | ||||
CAS No: | 853625-60-2 | 分子式: | C24H20N4O4S | 分子量: | 460.51 |
CAS No: | 853625-60-2 | ||||
分子式: | C24H20N4O4S | ||||
分子量: | 460.51 |
基本信息
产品编号:S10700 |
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产品名称:SecinH3 |
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CAS: |
853625-60-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
460.51 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
92mg/mL (199.78mM) |
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Ethanol |
1mg/mL warmed with 50ºC water bath (2.17mM) |
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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 |
2.1716mL |
10.8578mL |
21.7155mL |
5mM |
0.4343mL |
2.1716mL |
4.3431mL |
10mM |
0.2172mL |
1.0858mL |
2.1716mL |
50mM |
0.0434mL |
0.2172mL |
0.4343mL |
生物活性
产品描述 |
是 cytohesins 的拮抗剂,对于 hCyh1, hCyh2,mCyh3,hCyh3,drosophila steppke 和 yGea2-S7 的 IC50 值分别为 5.4μM,2.4μM,5.4μM,5.6μM,5.6μM 和 65μM。 |
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靶点/IC50 |
hCyh2 |
hCyh1 |
mCyh3 |
hCyh3 |
drosophila steppke |
2.4μM |
5.4μM |
5.4μM |
5.6μM |
5.6μM |
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体外研究 |
SecinH3 is a Sec7-specific guanine nucleotide exchange factor (GEF) inhibitor with preference for the small GEFs of the cytohesin family. SecinH3 almost completely blocks the insulin-dependent transcriptional repression of IGFBP1 with an IC 50 of 2.2μM. Insulin-stimulated translocation of ARF6 to the plasma membrane is also inhibited by SecinH3. It is found that SecinH3 inhibits the insulin-dependent phosphorylation of Akt and FoxO1A in a concentration-dependent manner. Insulininduced exclusion of FoxO1A from the nucleus is completely prevented by SecinH3. The binding of IRS1 to the insulin receptor is also inhibited by SecinH3. |
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体内研究 |
Compare to mice fed the same chow without SecinH3, the expression levels of the insulin-repressed gluconeogenic genes are elevated,whereas the insulin-induced glycolytic genes are reduced in SecinH3-treated mice. Insulin-stimulated Akt phosphorylation is also inhibited in SecinH3-treated mice. The expression of the genes for two key enzymes of mitochondrial β-oxidation, carnitine palmitoyltransferase 1a (Cpt1a) and hydroxyacyl-CoA dehydrogenase (Hadha), both of which are repressed by insulin, is increased in the SecinH3-treated mice. It is found significantly increased levels of serum insulin with slightly elevated glucose concentrations in SecinH3-treated mice. Accordingly, 3-hydoxybutyrate is increased in the serum of SecinH3-treated mice. |
推荐实验方法(仅供参考)
细胞实验: |
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105 HepG2 cells are seeded in 12 well plates and cultured for 24h in EMEM containing 10 % FCS. Cells are then serum starved in EMEM for 24h and stimulated for 12h with 10nM insulin in the presence of SecinH3, the negative control D5 or vehicle (0.2% final concentration of DMSO). Total mRNA is prepared using Kit and cDNA for qPCR is generated from 1μg RNA. qPCR is performed and data are normalized to β2-microglobulin expression. |
动物实验: |
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C57/Bl6N mice are kept on a 12h light/dark cycle in a pathogen-free animal facility and fed ad libitum with standard mice diet. After feeding with standard diet or with the same diet containing 0.9μmol/g SecinH3 for 3 days, mice are intraperitoneally injected with 100μL saline containing or not 40μg recombinant human insulin. After 10min the mice are anaesthetized and the liver is removed and lysed in lysis buffer. Normalized amounts of protein are either separated by SDSPAGE and transferred onto nitrocellulose, or immunoprecipitated using agarose-conjugated antibodies against IRβ or IRSI |
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 )