化合物 DAPT|T6202

價(jià)格	￥188	￥425	￥739
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱(chēng):化合物 DAPT	英文名稱(chēng):DAPT
CAS:208255-80-5	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.81%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T6202

Product Introduction

Bioactivity

名稱(chēng)	DAPT
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.
細(xì)胞實(shí)驗(yàn)	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(dòng)物實(shí)驗(yàn)	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].
體外活性	方法：卵巢腫瘤干細(xì)胞 (OCSC) HO8910 和 SKOV3 用 DAPT (1-20 μg/mL) 處理 24-72 h，使用 MTT 方法檢測(cè)細(xì)胞活力。結(jié)果：DAPT 孵育后，觀察到細(xì)胞自我更新和增殖顯著減少。DAPT 誘導(dǎo)對(duì) HO8910 和 SKOV3 OCSC 樣細(xì)胞的濃度依賴(lài)性抗增殖作用。[1] 方法：腫瘤細(xì)胞 GH3 和原代 GHoma 用 DAPT (20-100 nM) 處理 24 h，使用 Transwell 方法檢測(cè)細(xì)胞遷移情況。結(jié)果：DAPT 抑制 GH3 細(xì)胞和原代 GHoma 細(xì)胞遷移。[2]
體內(nèi)活性	方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 DAPT (1-5 mg/kg) 腹腔注射給攜帶大鼠垂體腫瘤 GH3 的 athymic immune-deficient nude 小鼠模型，每天一天，持續(xù)十五天。結(jié)果：DAPT 治療顯著抑制了腫瘤生長(zhǎng)。DAPT 治療的腫瘤中 Notch2 和 DLL3 的表達(dá)下調(diào)，DLL4 和 VEGF 表達(dá)沒(méi)有差異。[2] 方法：為研究對(duì)順鉑腎損傷的作用，將 DAPT (15 mg/kg in 20%Captisol) 腹腔注射給 cisplatin 引起腎損傷的 C57BL/6J 小鼠模型，每天一次，持續(xù)五天。結(jié)果：DAPT 減輕了順鉑誘導(dǎo)的腎小管損傷和腎小球?yàn)V過(guò)率的降低。Notch 信號(hào)通路可能是緩解順鉑化療相關(guān)腎臟并發(fā)癥的潛在治療靶點(diǎn)。[3]
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4.32 mg/mL (9.99 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. H2O : Insoluble DMSO : 43.2 mg/mL (100 mM)
關(guān)鍵字	Gamma secretase \| Amyloid-β \| DAPT \| Inhibitor \| Autophagy \| LY374973 \| Apoptosis \| Abeta \| LY 374973 \| Notch \| γ-secretase \| inhibit \| β-amyloid peptide
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相關(guān)庫(kù)	神經(jīng)保護(hù)化合物庫(kù) \| 抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 抗衰老化合物庫(kù) \| 蛋白酶抑制劑庫(kù) \| NO PAINS 化合物庫(kù) \| 神經(jīng)退行性疾病化合物庫(kù) \| Wnt/Hedgehog/Notch 通路化合物庫(kù) \| 細(xì)胞重編程化合物庫(kù)

關(guān)鍵字： LY-374973|||GSI-IX|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專(zhuān)業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷(xiāo)售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過(guò)在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過(guò)五百家學(xué)校和各類(lèi)企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

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