DAPT

カタログ番号 T6202 CAS 208255-80-5

別名: LY-374973, GSI-IX

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.

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DAPT, CAS 208255-80-5

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
5 mg	在庫あり	￥ 12,500
10 mg	在庫あり	￥ 21,000
25 mg	在庫あり	￥ 38,500
50 mg	在庫あり	￥ 67,500
100 mg	在庫あり	￥ 100,000
200 mg	在庫あり	￥ 125,000
500 mg	在庫あり	￥ 201,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 12,500

バルクのお問い合わせ

バッチを選択

純度: 99.81%

COA DATASHEET SDS HPLC HNMR

純度: 99.81%

COA DATASHEET SDS HNMR HPLC

純度: 99.79%

COA DATASHEET SDS HNMR HPLC

純度: 99.2%

COA DATASHEET SDS HNMR HPLC

純度: 98.06%

COA DATASHEET SDS HNMR HPLC

COA DATASHEET SDS

COA DATASHEET SDS HNMR

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	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.
ターゲット＆IC50	Aβ42:200 nM (in human primary neuronal cultures), β-Amyloid:115 nM (in human primary neuronal cultures), β-Amyloid:20 nM (HEK 293 cells)
In vitro	METHODS: Ovarian tumor stem cells (OCSC) HO8910 and SKOV3 were treated with DAPT (1-20 μg/mL) for 24-72 h. Cell viability was measured by MTT. RESULTS: A significant decrease in cell self-renewal and proliferation was observed after incubation with DAPT.DAPT induced a concentration-dependent antiproliferative effect on HO8910 and SKOV3 OCSC-like cells. [1] METHODS: Tumor cells GH3 and primary GHoma were treated with DAPT (20-100 nM) for 24 h. Cell migration was monitored using Transwell. RESULTS: DAPT inhibited the migration of GH3 cells and primary GHoma cells. [2]
In vivo	METHODS: To test the anti-tumor activity in vivo, DAPT (1-5 mg/kg) was injected intraperitoneally into an athymic immune-deficient nude mouse model harboring rat pituitary tumor GH3 one day a day for fifteen days. RESULTS: DAPT treatment significantly inhibited tumor growth, and the expression of Notch2 and DLL3 was down-regulated in DAPT-treated tumors, with no difference in the expression of DLL4 and VEGF. [2] METHODS: To investigate the effect on cisplatin-induced renal injury, DAPT (15 mg/kg in 20% Captisol) was administered intraperitoneally once daily for five days to a cisplatin-induced renal injury model in C57BL/6J mice. RESULTS: DAPT attenuated cisplatin-induced tubular injury and decreased glomerular filtration rate, and the Notch signaling pathway may be a potential therapeutic target for alleviating cisplatin chemotherapy-associated renal complications. [3]
キナーゼ試験	water content was 78.83 ± 0.35%. In DAPT group
細胞研究	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].
動物実験	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].

別名	LY-374973, GSI-IX
分子量	432.46
分子式	C23H26F2N2O4
CAS No.	208255-80-5

保存条件

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

溶解度情報

H2O: Insoluble

DMSO: 43.2 mg/mL (100 mM)

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.

引用文献

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.

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

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

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

DAPT

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords