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Umibecestat 是一种β-位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂,对人 BACE-1 和小鼠 BACE-1 的 IC50 分别为 11 nM 和 10 nM,可用于阿尔茨海默病的研究。
Umibecestat 是一种β-位点淀粉样前体蛋白裂解酶-1 (BACE-1) 抑制剂,对人 BACE-1 和小鼠 BACE-1 的 IC50 分别为 11 nM 和 10 nM,可用于阿尔茨海默病的研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,160 | 现货 | |
5 mg | ¥ 2,880 | 现货 | |
10 mg | ¥ 4,350 | 现货 | |
25 mg | ¥ 6,770 | 现货 | |
50 mg | ¥ 9,120 | 现货 | |
100 mg | ¥ 12,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 3,580 | 现货 |
产品描述 | Umibecestat is an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Umibecestat can be used for the research of alzheimer's disease. |
靶点活性 | BACE1 (mouse):10 nM , BACE1 (human):11 nM |
体外活性 | Umibecestat is a potent inhibitor of BACE-1 that is selective for BACE-1 over other human pepsin-like aspartic proteases, including BACE-2 and cathepsin D[1]. |
体内活性 | In both rat brain and CSF, Umibecestat (CNP520) (1.5-51.3 mg/kg; given by oral gavage; 72 hours) shows dose-dependent effects on Aβ40 and a long duration of action. Umibecestat (3.1 mg/kg; p.o.; 7 days) shows a > 75% reduction on Aβ40 and Aβ42 in CSF after dosing and returns slowly to baseline over the next 7 days[1]. |
别名 | CNP520 |
分子量 | 513.8 |
分子式 | C19H15ClF7N5O2 |
CAS No. | 1387560-01-1 |
Smiles | C[C@]1(CO[C@](C)(C(N)=N1)C(F)(F)F)c1nc(NC(=O)c2ncc(cc2Cl)C(F)(F)F)ccc1F |
密度 | 1.59 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: 95 mg/mL (184.90 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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