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PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).


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PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 2 mg | ¥ 2,480 | 5日内发货 | |
| 5 mg | ¥ 3,730 | 5日内发货 | |
| 25 mg | ¥ 13,900 | 10-14周 | |
| 50 mg | ¥ 18,300 | 10-14周 | |
| 1 mL x 10 mM (in DMSO) | ¥ 4,120 | 5日内发货 |
| 产品描述 | PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay). |
| 靶点活性 | BACE1:7.3 nM , BACE2:194 nM |
| 体外活性 | PF-06751979 shows improved selectivity over BACE2 (IC50=194 nM) in binding (27-fold) relative to the literature examples and across multiple chemical series in BACE1 program. |
| 体内活性 | PF-06751979 displays excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases including BACE2. Acute administration of PF-06751979 yields a robust dose-responsive and time-dependent reduction of cerebral spinal fluid (CSF) Aβx-40 with peak inhibition at 3 h of >77%.[1]. |
| 分子量 | 455.5 |
| 分子式 | C18H19F2N5O3S2 |
| CAS No. | 1818339-66-0 |
| 密度 | 1.66 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | Ethanol: 50 mg/mL (109.77 mM), Sonication is recommended. DMSO: 150 mg/mL (329.31 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.24 mM), Sonication is recommeded. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
对于不同动物的给药剂量换算,您也可以参考 更多