Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BACE1-IN-5 (Compound 15) 是一种 BACE1抑制剂,IC50为 9.1 nM。BACE1-IN-5还可抑制细胞 Aβ,IC50为 0.82 nM。并且,BACE1-IN-5 具有改善 hERG 抑制和 P-gp 外排的药物化学作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 10-14周 | ||
50 mg | ¥ 13,800 | 10-14周 | ||
100 mg | ¥ 17,500 | 10-14周 |
产品描述 | BACE1-IN-5 (Compound 15), a potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, demonstrates significant efficacy with an IC50 of 9.1 nM for BACE1 inhibition and an impressive IC50 of 0.82 nM against cellular amyloid-β (Aβ) production. Additionally, it is engineered to enhance hERG inhibition and P-gp efflux, indicating its optimized medicinal chemistry profile [1]. |
靶点活性 | BACE1:9.1 nM , Cellular β-Amyloid:0.82 nM |
体内活性 | BACE1-IN-5 (Compound 15; 1-3 mg/kg; oral administration; for 2-6 hours; male ICR mice) treatment causes a significant and dose-dependent decrease of total Aβ, reduces total Aβ by 76% (4 hours) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. BACE1-IN-5 demonstrats a K p,uu value of 1.3 at 1 mg/kg (4 hours time point). At 3 mg/kg, a maximum Aβ reduction of 87% is achieved at a free brain concentration of 9.5 ng/mL (21 nM) [1]. Animal Model: Male ICR mice [1] Dosage: 1 mg/kg, 3 mg/kg Administration: Oral administration; for 2 hours, 4 hours, and 6 hours Result: A significant and dose-dependent decrease of total Aβ was seen, reduced total Aβ by 76% (4 h) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. Demonstrats a K p,uu value close to 1 (K p,uu of 1.3) at 1 mg/kg (4 h time point). At 3 mg/kg, a maximum Aβ reduction of 87% was achieved at a free brain concentration of 9.5 ng/mL (21 nM). |
分子量 | 461.41 |
分子式 | C18H16F5N5O2S |
CAS No. | 2581114-83-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BACE1-IN-5 2581114-83-0 Neuroscience Beta Amyloid BACE BACE1IN5 BACE-1-IN-5 BACE1 IN 5 Inhibitor inhibitor inhibit