化合物 DAPT,DAPT
  • 化合物 DAPT,DAPT

化合物 DAPT|T6202

价格 188 739 1330 456 6790 3370 425 4780 2260
包装 1瓶 10瓶 25瓶 1瓶 500瓶 100瓶 5瓶 200瓶 50瓶
最小起订量 1瓶
发货地 上海
更新日期 2024-09-14
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产品详情

中文名称:化合物 DAPT英文名称:DAPT
CAS:208255-80-5品牌: TargetMol
产地: 美国保存条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格: 99.81%产品类别: 抑制剂
货号: T6202
2024-09-14 化合物 DAPT DAPT 1瓶/188RMB;10瓶/739RMB;25瓶/1330RMB;1瓶/456RMB;500瓶/6790RMB;100瓶/3370RMB;5瓶/425RMB;200瓶/4780RMB;50瓶/2260RMB 188 TargetMol 美国 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.81% 抑制剂

Product Introduction

Bioactivity

名称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.
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].
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]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : Insoluble
DMSO : 43.2 mg/mL (100 mM)
关键字Gamma secretase | Amyloid-β | DAPT | Inhibitor | Autophagy | LY374973 | Apoptosis | Abeta | LY 374973 | Notch | γ-secretase | inhibit | β-amyloid peptide
相关产品Guanidine hydrochloride | Naringin | Taurine | Gefitinib | Hydroxychloroquine | 5-Fluorouracil | Curcumin | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate
相关库神经保护化合物库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 抗衰老化合物库 | 蛋白酶抑制剂库 | NO PAINS 化合物库 | 神经退行性疾病化合物库 | Wnt/Hedgehog/Notch 通路化合物库 | 细胞重编程化合物库
关键字: LY-374973|||GSI-IX

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起,为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部,化学事业部,生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应;从商业化产品销售到个性化定制合成;从对明确靶点的分子筛选到对明确分子的多靶点筛选,从高通量筛选到化学结构优化,我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘,我们已成为筛选化合物领域优秀的供应商,为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛
成立日期 2013-04-18 (12年) 注册资本 566.2651万人民币
员工人数 100-500人 年营业额 ¥ 1亿以上
主营行业 化学试剂,生物活性小分子 经营模式 贸易,试剂,定制,服务
  • TargetMol中国(陶术生物)
VIP 12年
  • 公司成立:12年
  • 注册资本:566.2651万人民币
  • 企业类型:有限责任公司(自然人投资或控股)
  • 主营产品:小分子抑制剂,药物筛选化合物库,天然产物,活性分子化合物等
  • 公司地址:上海市闸北区江场三路28号4楼
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