Powder: -20°C for 3 years | In solvent: -80°C for 1 year
L-685458 (L-685,458) 是一种过渡状态模拟 γ-分泌酶抑制剂,抑制淀粉样 β-蛋白前体 γ-分泌酶活性,选择性高于其他检测的天冬氨酸蛋白酶 50-100 倍。它抑制 γ-分泌酶介导的 APP-C99 和 Notch-100 的裂解,可研究阿尔茨海默病和癌症。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
5 mg | ¥ 3,730 | 现货 | ||
10 mg | ¥ 5,450 | 现货 | ||
25 mg | ¥ 8,420 | 现货 | ||
50 mg | ¥ 11,300 | 现货 | ||
100 mg | ¥ 15,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,750 | 现货 |
产品描述 | L-685458 (L-685,458) is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM. |
靶点活性 | γ-secretase:17 nM(Ki) |
体外活性 | L-685,458 inhibits Aβ(40) formation in both Neuro2A and CHO cell lines overexpressing human AβPP695, and in SHSY5Y cells overexpressing the construct spβA4CTF with IC50 of 402 nM, 113 nM, and 48 nM, respectively, with the potency for reduction of Aβ(42) being about 2-fold lower. [1] In Tca8113 cells, L-685,458 inhibits cell growth by inducing G0–G1 cell cycle arrest and apoptosis. [2] In a T-cell acute lymphoblastic leukemia cell line, pre-treatment with L-685,458 enhances the anti-proliferative effect of imatinib. [3] L685,458 also significantly reduces HSV-1 replication in tissue culture by inhibiting signal peptide peptidase (SPP). [4] |
激酶实验 | HTRF Immunoassay for Aβ Quantitation: Homogeneous time-resolved fluorescence (HTRF) immunoassay methodology uses fluorescence resonance energy transfer (FRET) between two fluorophores, a donor EuK and a modified allophycocyanine pigment acceptor molecule, XL-665. When in proximity, nonradiative FRET takes place from nitrogen laser-excited EuK to XL-665, resulting in the emission of an amplified long-lived fluorescence signal. Briefly, in a typical 96-well plate assay, each well contains 0.75 nM antibody-EuK, 1.0 nM antibody-biotin, 2.0 nM SA-XL665, and 0.1?0.2 M potassium fluoride. Samples of conditioned cell culture medium or synthetic peptide standards and culture medium alone are added to give a total assay volume of 200 μL/well. Blank values are determined by the inclusion of 1.0 nM nonbiotinylated antibody in place of the biotinylated antibody. Following mixing, the reaction mixture is left at 4 °C to reach equilibrium binding, and then read on the Discovery HTRF microplate analyzer using the manufacturer's recommended settings. |
细胞实验 | The in vitro growth rate of Tca8113 cells treated with L-685,458, is measured by MTT. Briefly, Tca8113 cells are seeded in 96-well plates. On the day of harvest, 100 μL of spent medium is replaced with an equal volume of fresh medium containing 10% MTT 5 mg ml?1 stock. Plates are incubated at 37°C for 4 h, then 100 μl of DMSO is added to each well, and then plates are shaken at room temperature for 10 min. The absorbance is measured at 570 nm.(Only for Reference) |
别名 | L-685,458 |
分子量 | 672.85 |
分子式 | C39H52N4O6 |
CAS No. | 292632-98-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
Ethanol: 6 mg/mL
DMSO: 10.1 mg/mL(15 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.4862 mL | 7.4311 mL | 14.8622 mL | 37.1554 mL |
5 mM | 0.2972 mL | 1.4862 mL | 2.9724 mL | 7.4311 mL | |
10 mM | 0.1486 mL | 0.7431 mL | 1.4862 mL | 3.7155 mL |
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。
L-685458 292632-98-5 Apoptosis Neuroscience Proteases/Proteasome Stem Cells Gamma-secretase alzheimer’s disease inhibit HES1 L685458 cancer Inhibitor Gamma secretase L-685,458 L 685458 γ-secretase inhibitor