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DAPT

产品编号 T6202 CAS 208255-80-5

别名: LY-374973, GSI-IX

DAPT (LY-374973) 是一种 γ 分泌酶抑制剂，抑制总 Aβ 和 Aβ42 (IC50=115/200 nM)，具有口服活性。DAPT 也是一种 Notch 抑制剂。DAPT 可以诱导细胞分化、诱导细胞自噬和凋亡。

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DAPT, CAS 208255-80-5

规格	价格/CNY	货期
1 mg	￥ 189	现货
5 mg	￥ 426	现货
10 mg	￥ 739	现货
25 mg	￥ 1,330	现货
50 mg	￥ 2,260	现货
100 mg	￥ 3,380	现货
200 mg	￥ 4,820	现货
500 mg	￥ 6,790	现货
1 mL * 10 mM (in DMSO)	￥ 456	现货

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选择批次

纯度: 99.81%

COA DATASHEET SDS HNMR HPLC

纯度: 99.81%

COA DATASHEET SDS HNMR HPLC

纯度: 99.79%

COA DATASHEET SDS HNMR HPLC

纯度: 99.2%

COA DATASHEET SDS HNMR HPLC

纯度: 98.06%

COA DATASHEET SDS HNMR HPLC

COA DATASHEET SDS HPLC HNMR

COA DATASHEET SDS HNMR

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115/200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.
靶点活性	Aβ42:200 nM (in human primary neuronal cultures), β-Amyloid:115 nM (in human primary neuronal cultures), β-Amyloid:20 nM (HEK 293 cells)
体外活性	方法：卵巢肿瘤干细胞 (OCSC) HO8910 和 SKOV3 用 DAPT (1-20 μg/mL) 处理 24-72 h，使用 MTT 方法检测细胞活力。结果：DAPT 孵育后，观察到细胞自我更新和增殖显著减少。DAPT 诱导对 HO8910 和 SKOV3 OCSC 样细胞的浓度依赖性抗增殖作用。[1] 方法：肿瘤细胞 GH3 和原代 GHoma 用 DAPT (20-100 nM) 处理 24 h，使用 Transwell 方法检测细胞迁移情况。结果：DAPT 抑制 GH3 细胞和原代 GHoma 细胞迁移。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 DAPT (1-5 mg/kg) 腹腔注射给携带大鼠垂体肿瘤 GH3 的 athymic immune-deficient nude 小鼠模型，每天一天，持续十五天。结果：DAPT 治疗显著抑制了肿瘤生长。DAPT 治疗的肿瘤中 Notch2 和 DLL3 的表达下调，DLL4 和 VEGF 表达没有差异。[2] 方法：为研究对顺铂肾损伤的作用，将 DAPT (15 mg/kg in 20%Captisol) 腹腔注射给 cisplatin 引起肾损伤的 C57BL/6J 小鼠模型，每天一次，持续五天。结果：DAPT 减轻了顺铂诱导的肾小管损伤和肾小球滤过率的降低。Notch 信号通路可能是缓解顺铂化疗相关肾脏并发症的潜在治疗靶点。[3]
细胞实验	Human embryonic kidney cells, transfected with the gene for APP751 (HEK 293) were used for routine Ab reduction assays. The Ab peptides secreted from these cells have been characterized previously. Cells were plated in 96-well plates and allowed to adhere overnight in Dulbecco's modified Eagle medium (DMEM) supplemented with 10% heat-inactivated fetal bovine serum. For compound screening and dose±response testing, compounds were diluted from stock solutions in DMSO to yield a final concentration equal to 0.1% DMSO in media. Cells were pre-treated for 2 h at 378C with compounds, media were aspirated off and fresh compound solutions applied. After an additional 2-h treatment period, conditioned media were drawn off and analyzed by a sandwich ELISA (266±3D6) specific for total Ab. Reduction of Ab production was measured relative to control cells treated with 0.1% DMSO and expressed as percentage inhibition. Data from at least six doses in duplicate were fitted to a four-parameter logistical model using XLfit software in order to determine potency [1].
动物实验	All studies were conducted with three- to four-month-old heterozygous PDAPP transgenic mice overexpressing the APPV717F a mutant form of the amyloid precursor protein. These animals have been previously shown to exhibit many of the neuropathological features of AD and to produce high levels of Ab in a regionally specific manner. Each treatment group (n=10) consisted of equal numbers of age-matched male and female animals that were fasted overnight prior to treatment. Both treatment and control groups were dosed at a volume of 10 mL/kg with compound formulated in corn oil, 5% (v/v) ethanol or vehicle alone. Tissues were processed and all Ab and APP measurements were made as described previously. After removal of the brain, the cortex from one hemisphere was homogenized, extracted with 5 M guanidine, 50 mM Tris ± pH 8.0, centrifuged, and the supernatant was used for Ab measurements. Cortex from the other hemisphere was snap frozen for analysis of compound levels. Ab levels were expressed as ng/g of wet tissue weight, and percentage reductions were calculated relative to the mean Ab level of tissue from vehicle-treated control animals. Data were analyzed with Mann± Whitney non-parametric statistics to assess significance [1].

别名	LY-374973, GSI-IX
化合物与蛋白结合的复合物	Cryo-EM structure of gamma secretase in complex with a drug DAPT
分子量	432.46
分子式	C23H26F2N2O4
CAS No.	208255-80-5

存储

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

溶解度

H2O: Insoluble

DMSO: 43.2 mg/mL (100 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	1 mM	2.3124 mL	11.5618 mL	23.1235 mL	57.8088 mL
	5 mM	0.4625 mL	2.3124 mL	4.6247 mL	11.5618 mL
	10 mM	0.2312 mL	1.1562 mL	2.3124 mL	5.7809 mL
	20 mM	0.1156 mL	0.5781 mL	1.1562 mL	2.8904 mL
	50 mM	0.0462 mL	0.2312 mL	0.4625 mL	1.1562 mL
	100 mM	0.0231 mL	0.1156 mL	0.2312 mL	0.5781 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Jiang LY, et al. γ-Secretase Inhibitor, DAPT Inhibits Self-renewal and Stemness Maintenance of Ovarian Cancer Stem-like Cells In Vitro. Chin J Cancer Res. 2011 Jun;23(2):140-6. 2. Feng J, et al. DAPT, a γ-Secretase Inhibitor, Suppresses Tumorigenesis, and Progression of Growth Hormone-Producing Adenomas by Targeting Notch Signaling. Front Oncol. 2019 Aug 27;9:809. 3. Soni H, et al. γ-secretase inhibitor DAPT mitigates cisplatin-induced acute kidney injury by suppressing Notch1 signaling. J Cell Mol Med. 2019 Jan;23(1):260-270. 6. Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128(1):483-499. 7. Yixin Tao, et al. β-catenin activation in hair follicle dermal stem cells induces ectopic hair outgrowth and skin fibrosis. J Mol Cell Biol. 2018 May 16. 8. Zhou Y, Li X. LxA4 Inhibits LPS Induced Proinflammatory Response and Microglia Polarization through Notch Signaling Pathway[J]. Revista Argentina de Clínica Psicológica. 2021, 30(1): 330. 9. Huang C, Yan T, Xu Z, et al. Hypoxia Enhances Fusion of Oral Squamous Carcinoma Cells and Epithelial Cells Partly via the Epithelial–Mesenchymal Transition of Epithelial Cells[J]. BioMed research international. 2018 Feb 8;2018:5015203. 10. Zhenyu Wang, Weijian Li, Hongshu Jing, Ming Ding, Gong-Bo Fu, Tianjie Yuan, Weijian Huang, Mengjun Dai, Dan Tang, Min Zheng, Yi Chen, Hongdan Zhang, Yuan Peng, Qigen Li, Weifeng Yu, Hexin Yan, Bo Zhai . Generation of hepatic spheroids using human hepatocyte-derived liver progenitor-like cells for hepatotoxicity screening. Theranostics.

文献引用

1. Wang Z, Li W, Jing H, et al. Generation of hepatic spheroids using human hepatocyte-derived liver progenitor-like cells for hepatotoxicity screening. Theranostics. 2019, 9(22): 6690 2. Cai N, Xu B, Li X, et al. Roflumilast, a cyclic nucleotide phosphodiesterase 4 inhibitor, protects against cerebrovascular endothelial injury following cerebral ischemia/reperfusion by activating the Notch1/Hes1 pathway. European Journal of Pharmacology. 2022: 175027 3. Huang C, Yan T, Xu Z, et al. Hypoxia Enhances Fusion of Oral Squamous Carcinoma Cells and Epithelial Cells Partly via the Epithelial–Mesenchymal Transition of Epithelial Cells. BioMed Research International. 2018 Feb 8;2018:5015203 4. Yang L, Wang X, Zhao G, et al.Leveraging temporal Wnt signal for efficient differentiation of intestinal stem cells in an organoid model.Stem Cells and Development.2023 (ja). 5. Qu R, Peng Y, Zhou M, et al.MiR-223-3p attenuates M1 macrophage polarization via suppressing the Notch signaling pathway and NLRP3-mediated pyroptosis in experimental autoimmune uveitis.European Journal of Pharmacology.2023, 960: 176139.

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

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

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。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

DAPT 208255-80-5 Apoptosis Autophagy Neuroscience Proteases/Proteasome Stem Cells Beta Amyloid Gamma-secretase Gamma secretase Amyloid-β Inhibitor LY-374973 LY374973 Abeta LY 374973 Notch γ-secretase inhibit β-amyloid peptide GSI-IX inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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DAPT

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords