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SecinH3.
Sec7特异性GEF抑制剂。SecinH3 是 cytohesins 的拮抗剂,对于 hCyh1, hCyh2,mCyh3,hCyh3,drosophila steppke 和 yGea2-S7 的 IC50 值分别为 5.4 μM,2.4 μM,5.4 μM,5.6 μM,5.6 μM 和 65 μM。
目录号: PC16855 纯度: ≥98%
CAS No. :853625-60-2
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中文名称
SecinH3.
中文别名
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
英文名称
SecinH3
英文别名
N-[4-[5-(1,3-benzodioxol-5-yl)-3-methoxy-1,2,4-triazol-1-yl]phenyl]-2-phenylsulfanylacetamide;SecinH3;Cytohesins Inhibitor SecinH3;N-(4-(5-(1,3-Benzodioxol-5-yl)-3-methoxy-1H-1,2,4-triazol-1-yl)phenyl)-2-(phenylthio)acetamide;AC1LJQ5K;SureCN7899934;CTK8E9012;HMS2211A12;IN1100;N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE;Secin H3;N-[4-[5-(1,3-benzodioxol-5-yl)-3-methoxy-1,2,4-triazol-1-yl]phenyl]-2-(phenylthio)acetamide;N-{4-[5-(2H-1,3-benzodioxol-5-yl)-3-methoxy-1H-1,2,4-triazol-1-yl]phenyl}-2-(phenylsulfanyl)acetamide;Secin-H3; Secin H3;N-[4-[5-(1,3-benzodioxol-5-yl)-3-methox
Cas No.
853625-60-2
分子式
C24H20N4O4S
分子量
460.51
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

SecinH3 is an antagonist of cytohesins with IC50s of 5.4 μM, 2.4 μM, 5.4 μM, 5.6 μM, 5.6 μM and 65 μM for hCyh1, hCyh2, mCyh3, hCyh3, drosophila steppke and yGea2-S7, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 5.4 μM (hCyh1),2.4 μM (hCyh2),5.4 μM (mCyh3),5.6 μM (hCyh3),5.6 μM (drosophila steppke), 65 μM (yGea2-S7)

体外研究(In Vitro)

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 IC50 of 2.2 μM. 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. Insulin-induced exclusion of FoxO1A from the nucleus is completely prevented by SecinH3. The binding of IRS1 to the insulin receptor is also inhibited by SecinH3.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 130 mg/mL (282.30 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1715 mL 10.8575 mL 21.7151 mL
5 mM 0.4343 mL 2.1715 mL 4.3430 mL
10 mM 0.2172 mL 1.0858 mL 2.1715 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 3.25 mg/mL (7.06 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (7.06 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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