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LY2886721 是选择性的,口服活性的 β 位淀粉样蛋白前体蛋白裂解酶 1 抑制剂,对重组人 BACE1的 IC50=20.3 nM。它对 BACE1的选择性高于对组织蛋白酶 D、胃蛋白酶、肾素的选择性,但缺乏对 BACE2的选择性。它可透过血脑屏障,并可用于研究阿尔茨海默氏病。
LY2886721 是选择性的,口服活性的 β 位淀粉样蛋白前体蛋白裂解酶 1 抑制剂,对重组人 BACE1的 IC50=20.3 nM。它对 BACE1的选择性高于对组织蛋白酶 D、胃蛋白酶、肾素的选择性,但缺乏对 BACE2的选择性。它可透过血脑屏障,并可用于研究阿尔茨海默氏病。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 170 | 现货 | |
5 mg | ¥ 398 | 现货 | |
10 mg | ¥ 678 | 现货 | |
25 mg | ¥ 1,310 | 现货 | |
50 mg | ¥ 2,370 | 现货 | |
100 mg | ¥ 3,390 | 现货 | |
200 mg | ¥ 4,730 | 现货 |
产品描述 | LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease. |
靶点活性 | BACE1:20.3 nM, BACE2:10.2 nM |
体外活性 | LY2886721 is an oral, small molecule of β-site amyloid protein cleaving enzyme (BACE) inhibitor with the potential to inhibit the synthesis of β-amyloid and thereby to slow the Clinicalal progression of AD. [1] LY2886721 can also targetγ-secretase to nhibit the synthesis of β-amyloid. [2] |
激酶实验 | The CTLs and NK cells (0.8×106/mL) are treated with the inhibitors L1 (10-20 μM) or Aloxistatin (20-30 μM) for 24 hr at 37°C in 24-well plates. Cells are then used in 51Cr-release assays or are lysed to examine perforin in Western blots. The inhibitor is also added at the same concentration during the 4 hr reactions in some 51Cr-release assays, as indicated. Cell lysates are prepared using NP-40 lysis buffer (25 mM HEPES, 250 mM NaCl, 2.5 mM ethylenediaminetetraacetic acid, 0.1% volume/volume Nonidet P-40) and total protein concentration is determined using the Bradford assay. Equal amounts of protein are loaded and resolved on 8% SDS-PAGE gels. Human or mouse perforin is detected using the appropriate antibodies as indicated. Anti-actin antibody is used as a loading control[2]. |
分子量 | 390.41 |
分子式 | C18H16F2N4O2S |
CAS No. | 1262036-50-9 |
Smiles | NC1=N[C@]2(COC[C@H]2CS1)c1cc(NC(=O)c2ccc(F)cn2)ccc1F |
密度 | 1.57 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 1 mg/ml, Sonication is recommended. |
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