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LY-411575

LY-411575

产品编号 T6063   CAS 209984-57-6
别名: LY411575

LY-411575 是一种高效的γ-secretase 抑制剂,能够抑制 Aβ40 蛋白的产生,在膜中的 IC50 为 0.078 nM,在细胞中为 0.082 nM。 它还抑制 Notch 切割,IC50 为 0.39 nM。

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LY-411575 Chemical Structure
LY-411575, CAS 209984-57-6
规格 价格/CNY 货期 数量
1 mg ¥ 338 现货
2 mg ¥ 482 现货
5 mg ¥ 822 现货
10 mg ¥ 1,370 现货
25 mg ¥ 2,320 现货
50 mg ¥ 3,460 现货
100 mg ¥ 4,920 现货
1 mL * 10 mM (in DMSO) ¥ 869 现货
产品目录号及名称: LY-411575 (T6063)
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纯度: 99.38%
纯度: 98.35%
纯度: 97.03%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 LY-411575, a potent γ-secretase inhibitor, is with IC50 of 0.078 nM in the membrane and 0.082 nM in cell-based. It also suppresses Notch clevage with IC50 of 0.39 nM.
靶点活性 Notch S3 cleavage:0.39 nM, γ secretase (cell-based):0.082 nM, γ secretase (membrane-based):0.078 nM
体外活性 LY-411575 inhibits γ-secretase which can be assessed by the substrates like amyloid precursor protein (APP) and Notch S3 cleavage. [1] LY-411575, which blocks Notch activation, results in apoptosis in primary and immortalized KS cells. [2]
体内活性 10 mg/kg oral dose of LY-411575 decreases brain and plasma Aβ40 and -42 dose-dependently. [1] LY-411575 reduces cortical Aβ40 in young (preplaque) transgenic CRND8 mice (ED50 ≈ 0.6 mg/kg) and produces significant thymus atrophy and intestinal goblet cell hyperplasia at higher doses (>3 mg/kg). The therapeutic window is similar after oral and subcutaneous administration and in young and aged CRND8 mice. Both the thymus and intestinal side effects are reversible after a 2-week washout period. Three-week treatment with 1 mg/kg LY411575 reduces cortical Aβ40 by 69% without inducing intestinal effects, although a previously unreported change in coat color is observed. [3]
激酶实验 Assays for Aβ and NICD: Procedures for measuring γ-secretase activity in membranes prepared from HEK293 cells expressing APP have been described previously (Zhang L et al Biochemistry 40, 5049-5055). Intact HEK293 cells expressing either APP or NΔE are treated with various concentrations of LY- 411,575 for 4 hours at 37 °C. In the case of cells expressing NΔE, cells are lysed, the cell lysates are separated on a 4-12% NuPAGE gel, and the processed NICD fragment is detected via Western blot with a cleavage site-specific antibody. The inhibition of NICD production is quantified by spot densitometric analysis using FluorChem. In the case of cells expressing APP, the conditioned medium is collected, centrifuged at 10,000 × g for 5 minutes to remove cell debris, and stored at -20 °C prior to the determination of Aβ levels. Aβ40 and -42 produced in HEK293 membrane- and cell-based assays, as well as plasma Aβ40 and cortex Aβ40 from TgCRND8 mice, are analyzed without pretreatment using an electrochemiluminescence detection-based immunoassay. Plasma Aβ42 is measured by enzyme-linked immunosorbent assay. A commercially available enzyme-linked immunosorbent assay kit is used to measure cortex Aβ42 according to the manufacturer''s instructions.
细胞实验 DNA/PI staining is performed using standard methodologies. Briefly, 1 &times; 106 cells are permeabilized with 100% ethanol in the presence of 15% FBS. The cells are washed and then treated for 15 minutes at 37 °C with 10 mg/mL RNAse. PI (5 mg/mL) is added, and the cells incubated for 1 hour at 4 °C prior to analysis by flow cytometry with 10 000 cells analysed per gated determination. The results are confirmed using the Immunotech Annexin V staining kit following the manufacturers&rsquo; instructions. At least three independent experiments are performed showing similar results.</(Only for Reference)
别名 LY411575
分子量 479.48
分子式 C26H23F2N3O4
CAS No. 209984-57-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 88 mg/mL (183.5 mM)

Ethanol: 11 mg/mL (22.9 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.0856 mL 10.428 mL 20.8559 mL 52.1398 mL
5 mM 0.4171 mL 2.0856 mL 4.1712 mL 10.428 mL
10 mM 0.2086 mL 1.0428 mL 2.0856 mL 5.214 mL
20 mM 0.1043 mL 0.5214 mL 1.0428 mL 2.607 mL
DMSO 50 mM 0.0417 mL 0.2086 mL 0.4171 mL 1.0428 mL
100 mM 0.0209 mL 0.1043 mL 0.2086 mL 0.5214 mL

计算器

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参考文献

1. Wong GT, et al, J Biol Chem, 2004, 279(13), 12876-12882. 2. Curry CL, et al, Oncogene, 2005, 24(42), 6333-6344. 3. Hyde LA, et al, J Pharmacol Exp Ther, 2006, 319(3), 1133-1143. 4. Yang D L, Zhang Y, He L, et al. Demethylzeylasteral (T-96) Initiates Extrinsic Apoptosis Against Prostate Cancer cells by Inducing ROS-Mediated ER Stress and Suppressing Autophagic Flux[J]. 2021

文献引用

1. Yang D L, Zhang Y, He L, et al. Demethylzeylasteral (T-96) Initiates Extrinsic Apoptosis Against Prostate Cancer cells by Inducing ROS-Mediated ER Stress and Suppressing Autophagic Flux. Biological Research. 2021, 54(1): 1-14. 2. Zhang S, Lou H, Lu H, et al.Characterization of Proliferation Medium and Its Effect on Differentiation of Muscle Satellite Cells from Larimichthys crocea in Cultured Fish Meat Production.Fishes.2023, 8(9): 429.
Daunorubicin hydrochloride Nortriptyline hydrochloride Dehydrotrametenolic acid XST-14 COG-1410 acetate Luteolin Calycosin 1-beta-D-Arabinofuranosylthymine

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 已知活性化合物库 神经再生化合物库 抗结直肠癌化合物库 HIF-1化合物库 神经元分化化合物库 癌细胞分化化合物库 蛋白酶抑制剂库 抗衰老化合物库 NO PAINS 化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

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。

Keywords

LY-411575 209984-57-6 Apoptosis Neuroscience Proteases/Proteasome Stem Cells Gamma-secretase Inhibitor Gamma secretase γ-secretase Notch LY411575 LY 411575 inhibit inhibitor

 

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