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DAPT

目录号 M1746 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


DAPT (GSI-IX)是一种新型γ-分泌酶抑制剂,抑制HEK 293细胞中全部Aβ产量, IC50为20 nM。

DAPT结构式

别名:GSI-IX

包装 价格 库存状态
10mM*1mL 原价 ¥ 585
促销价 ¥ 555.75
中国库存现货
10mg 原价 ¥ 765
促销价 ¥ 726.75
中国库存现货
50mg 原价 ¥ 2520
促销价 ¥ 2394
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
生物活性

DAPT (GSI-IX)是一种新型γ-分泌酶抑制剂,抑制HEK 293细胞中全部Aβ产量, IC50为20 nM。DAPT功能性抑制γ-分泌酶而降低HEK 293细胞中全部Aβ产量,IC50为20 nM。DAPT作用于原代培养的人神经细胞,也抑制Aβ产量,作用于全部Aβ和Aβ42时, IC50分别为115 nM和200 nM,比作用于HEK 293细胞时低5-10倍。最新研究显示DAPT 抑制SK-MES-1 细胞增殖,这种作用存在浓度依赖性,IC50为11.265 μM。

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 SK-MES-1
方法 Cells are seeded into 96-well plates and exposed to 0.1% DMSO or DAPT at concentrations in the range of 2.5 μM–160 μM for 72 hours. Cytotoxicity is determined with 3-(4, 5)-dimethylthiahiazo-(-z-y1)-3, 5-di-phenytetrazoliumromide (MTT) dye reduction assay with minor modifications. Briefly, after incubation with DAPT, 20 μL MTT solution (5 mg/mL in PBS) is added to 180 μL medium in each well and plates are incubated for 4 hours at 37 °C, and subsequently 150 μL DMSO is added to each well, and mixed by shaking at room temperature for 15 minutes. Absorption is measured by an enzyme-linked immunosorbent assay at 490 nm to determine absorbance values.
浓度 2.5 ~ 160 μM
处理时间 72 h
动物实验
动物模型 MCAO rat model
配制 prepared by dissolving DAPT powder in 0.01 M phosphate-buffered saline containing 5% dimethyl sulfoxide (Fisher Scientific, Fair Lawn, NJ, USA).
剂量 1 μg/μl
给药处理 The solution was filtered and stereotactically injected into the right cerebral ventricle using the following coordinates: −0.8 mm anteroposterior, ±1.5 mm mediolateral, and −4.5 mm dorsoventral from the bregma.
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 432.46
分子式 C23H26F2N2O4
CAS号 208255-80-5
纯度 98.36%
溶解性(25°C) DMSO 76 mg/mL
储存和运输条件 固体粉末: -20°C 冷藏长期储存
常温运输及临时存放
储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.3124 mL 11.5618 mL 23.1235 mL
5 mM 0.4625 mL 2.3124 mL 4.6247 mL
10 mM 0.2312 mL 1.1562 mL 2.3124 mL
使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 Oncol Lett (2017). Figure 6. DAPT (AbMole BioScience, Shanghai, China)
方法 Co‑IP assay
细胞系 SMMC‑7721 cells
浓度 1 μM
处理时间
实验结果 The interaction between Jagged1 and Notch1 in SMMC‑7721 cells was also significantly reduced after adding DAPT compared with that of the normal serum group (P<0.01) (Fig. 6).
数据来源 Oncol Lett (2017). Figure 5. DAPT (AbMole BioScience, Shanghai, China)
方法 Western blot
细胞系 SMMC‑7721 cells
浓度 1 μM
处理时间
实验结果 The levels of Jagged1 and Notch1 were decreased after adding the Notch inhibitor, DAPT, indicating that DAPT successfully inhibited the Jagged1/Notch signaling pathway. In addition, the expression of VEGF protein was reduced after adding DAPT (Fig. 5).
数据来源 Circ Res (2017). Figure 2. DATP (Abmole Bioscience)
方法 Retina dissection and whole mount staining
细胞系 mice
浓度 100 mg/kg
处理时间
实验结果 DAPT treatment resulted in a large increase in vessel density and expansion of the vascular plexus in the postnatal retina of control mice (Fig. 2A, C, E, G). DAPT completely rescued the defect in SENP1-ecKO pups (Fig. 2B, D, F, H), which resulted in vascular length, vascular coverage, and tip sprouts growth comparable to the control group (Fig. 2I-K).
数据来源 Sci adv (2015). Figure 5. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
方法 Immunohistochemistry
细胞系
浓度 100 mg/kg, daily
处理时间
实验结果 "The PlGF-modulated opposing vascular effects in relation to Dll4-Notch inhibition alter tumor growth by changing the microenvironment, tumor cell proliferation, and apoptosis."
数据来源 Sci adv (2015). Figure 4. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
方法 human tumor models, Immunohistochemistry
细胞系
浓度 100 mg/kg, daily
处理时间
实验结果 PlGF mediates opposing vascular effects in nontreated and Dll4-Notch inhibitor–treated mouse tumors.
数据来源 Sci adv (2015). Figure 3. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
方法 Immunohistochemistry
细胞系 Human JE-3, BeWo, MDA-MB-231 cells
浓度 100 mg/kg, daily
处理时间
实验结果 "Both terminal deoxynucleotidyl transferase–mediated deoxyuridine triphosphate nick end labeling (TUNEL) staining and measurements of the activated or cleaved caspase 3 showed reductions of apoptotic cells in Dll4-Notch inhibitor–treated JE-3 and BeWo tumors. In contrast, treatment of PlGF-negative MDAMB-231 tumors with DAPT and Dll4 blockade showed completely opposite effects on cell proliferation and apoptosis, tipping the balance toward an apoptotic phenotype."
数据来源 Sci adv (2015). Figure 1. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
方法 Immunohistochemistry
细胞系 Human JE-3, BeWo, MDA-MB-231 cells
浓度 100 mg/kg, daily
处理时间
实验结果 "PlGF expression determines opposing effects of Dll4-Notch inhibition on human tumor growth and vascular remodeling."
参考文献

A New Strategy for Discontinuation of Dual Antiplatelet Therapy: The RESET Trial (REal Safety and Efficacy of 3-month dual antiplatelet Therapy following Endeavor zotarolimus-eluting stent implantation).
Kim BK et al. J Am Coll Cardiol. 2012 Sep 5. PMID: 22999717.

Stent thrombosis: insights on outcomes, predictors and impact of dual antiplatelet therapy interruption from the SPIRIT II, SPIRIT III, SPIRIT IV and COMPARE trials.
Kedhi E et al. EuroIntervention. 2012 Sep 20;8(5):599-606. PMID: 22995087.

The γ-secretase inhibitor DAPT increases the levels of gangliosides at neuritic terminals of differentiating PC12 cells.
Oikawa et al. Neurosci Lett. 2012 Sep 6;525(1):49-53. PMID: 22867970.

Gamma-secretase inhibitor DAPT suppresses glioblastoma growth via uncoupling of tumor vessel density from vessel function.
Zou et al. Clin Exp Med. 2012 Jul 27. PMID: 22836313.

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关键词:DAPT, GSI-IX, DAPT供应商, Gamma-secretase抑制剂, 购买DAPT, DAPT结构式

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