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Lanabecestat (AZD3293) 是一种具有高效性和高渗透性、口服活性且可穿过血脑屏障的 BACE1 抑制剂(Ki:0.4 nM),Lanabecestat 可用于研究像阿尔茨海默症类的神经系统疾病。
Lanabecestat (AZD3293) 是一种具有高效性和高渗透性、口服活性且可穿过血脑屏障的 BACE1 抑制剂(Ki:0.4 nM),Lanabecestat 可用于研究像阿尔茨海默症类的神经系统疾病。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 799 | 现货 |
产品描述 | Lanabecestat (AZD3293) is a highly potent and highly permeable, orally active BACE1 inhibitor (Ki: 0.4 nM) that crosses the blood-brain barrier, Lanabecestat can be used for the study of neurological diseases like Alzheimer's disease. |
靶点活性 | BACE1:0.4 nM (cell free), BACE1:0.4 nM |
体外活性 | Lanabecestat 差异性地改变了 5xFAD 和 APP KI小鼠的小胶质细胞蛋白水平[1]。 |
体内活性 | Lanabecestat 治疗(1 mg/kg;口服灌胃;每天一次;持续 3 周)能在 4-AP 细胞发生模型中增加了 Bace1-null 小鼠的爆发频率[1]。 |
细胞实验 | Cells are incubated with different Lanabecestat concentrations for 5 to 16?h, and the release of sAβPPβ, Aβ1-40, Aβ1-42, or sAβPPα into the medium is analyzed using kits. Cytotoxic effect of Lanabecestat is evaluated in the cell plates using cell proliferation/cytotoxicity kit. |
动物实验 | Female 7- to 14-week-old C57BL/6 mice (n=6 per treatment group and time point) receive a vehicle or Lanabecestat solution at 50, 100, or 200 μmol/kg (20, 41, or 82?mg/kg) as a single dose via oral gavage. Mice and guinea pigs are anesthetized 1.5, 2, 3, 4, 6, 8, 16, 24, or 48?h after the (last) administration of vehicle or drug and are then kept under isoflurane anesthesia. Cerebrospinal fluid (CSF) is aspirated from the cisterna magna, and plasma is isolated from blood collected by cardiac puncture into EDTA tubes. The animals are then sacrificed by decapitation, and the brains are dissected into hemispheres. |
别名 | LY3314814, AZD3293 |
分子量 | 412.53 |
分子式 | C26H28N4O |
CAS No. | 1383982-64-6 |
Smiles | COC1CCC2(Cc3ccc(cc3[C@@]22N=C(C)C(N)=N2)-c2cncc(c2)C#CC)CC1 |
密度 | 1.23 g/cm3 (Predicted) |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 80 mg/mL (193.92 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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