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同义名 : | - |
CAS号 : | 102636-74-8 | |
货号 : | A1145760 | |
分子式 : | C23H29N3O3 | |
纯度 : | 98% (HPLC) | |
分子量 : | 395.49 | |
MDL号 : | MFCD00288296 | |
存储条件: |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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描述 | CINPA1 is a selective CAR (Constitutive androstane receptor) with IC50 value of ~70nM for inhibition of CAR-mediated gene expression in primary human hepatocytes. It showed no activity on PXR and did not alter the protein levels or subcellular localization of CAR. CINPA1 attenuated CAR-mediated gene expression, including CYP2B6 and CYP3A4 at concentration of 1μM or 5μM at different cells expressing CAR post 24h or 48h. | ||
作用机制 | CINPA1 could reside in the ligand-binding pocket to stabilize the CAR-LBD (ligand-binding domain) in a more rigid, less fluid state and disrupt CAR binding to the DNA response elements at promoter regions of target gene.[1][2] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.53mL 0.51mL 0.25mL |
12.64mL 2.53mL 1.26mL |
25.29mL 5.06mL 2.53mL |
参考文献 |
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