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E1231 是 SIRT1 的激活剂。 E1231 通过增强 ABCA1 表达来防止实验性动脉粥样硬化并降低血浆胆固醇和甘油三酯。
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E1231 是 SIRT1 的激活剂。 E1231 通过增强 ABCA1 表达来防止实验性动脉粥样硬化并降低血浆胆固醇和甘油三酯。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 282 | 现货 | |
5 mg | ¥ 696 | 现货 | |
10 mg | ¥ 1,090 | 现货 | |
25 mg | ¥ 2,190 | 现货 | |
50 mg | ¥ 3,210 | 现货 | |
100 mg | ¥ 4,510 | 现货 | |
500 mg | ¥ 8,880 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 768 | 现货 |
产品描述 | E1231 is an activator of SIRT1 . E1231 protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression. |
体外活性 | E1231,一种哌嗪1,4-二酰胺化合物,被确认为SIRT1激活剂,其EC50值为0.83 μM。E1231与重组人SIRT1蛋白相互作用,并去乙酰化肝脏X受体-α (LXRα)。依赖于SIRT1和LXRα,E1231在RAW 264.7细胞中增加ATP结合盒转运蛋白A1 (ABCA1)的表达。通过SIRT1和ABCA1,E1231促进胆固醇外排并抑制RAW 264.7细胞中的脂质积累。在金黄仓鼠高脂血症模型中,E1231治疗降低了血清和肝脏中的总胆固醇和甘油三酯水平,同时增加了粪便中的胆固醇含量。此外,E1231增加了肝脏中ABCA1和SIRT1蛋白的表达。在ApoE-/-小鼠中,E1231治疗与未治疗的ApoE-/-小鼠相比,减少了动脉粥样硬化斑块的发展。 |
细胞实验 | A high-throughput screening assay was established to identify SIRT1 activators. Surface plasmon resonance and immunoprecipitation were performed to confirm the interaction of E1231 with SIRT1. Cholesterol assay was performed to demonstrate the in vitro effect of E1231. The in vivo effect of E1231 was evaluated in experimental models |
分子量 | 363.41 |
分子式 | C21H21N3O3 |
CAS No. | 1031195-19-3 |
Smiles | C(=O)(C=1C2=C(N=C(C1)C=3OC(C)=CC3)C=CC=C2)N4CCN(C(C)=O)CC4 |
密度 | 1.259 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 60 mg/ml (165.1 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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