上海陌孚医药科技有限公司

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