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DAPT

GSI-IX,LY-374973

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

目录号
EY0866
EY0866
EY0866
EY0866
纯度
99.28%
99.28%
99.28%
99.28%
规格
5 mg
10 mg
25 mg
50 mg
原价
400
500
1300
2000
售价
400
500
1300
2000
库存
现货
现货
现货
现货
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  • 生物活性

    DAPT is a potent and specific inhibitor of γ-secretase. It has been shown to cause a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ40 and Aβ42 respectively). There is evidence that DAPT does not effect APPα and APPβ levels. It mimics notch signaling deficiencies at morphological, molecular and biochemical levels and has been shown to block notch signaling in hybrid human-mouse foetal thymus organ culture (FTOC).

  • 体外研究

  • 体内研究

    5% DMSO+95% Corn oil

  • 激酶实验

  • 细胞实验

  • 动物实验

    ≤100 mg/kg 口服处理

  • 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）

    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，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Dovey HF, et al. J Neurochem. 2001, 76(1), 173-181.
    [2] Lanz, Thomas A., et al., 2003. The gamma-secretase inhibitor N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester reduces A beta levels in vivo in plasma and cerebrospinal fluid in young (plaque-free) and aged (plaque-bearing) Tg2576 mice. The Journal of pharmacology and experimental therapeutics. 305(3): 864-71.
    [3] Gowrishankar, Kavitha., et al., 2004. Release of a membrane-bound death domain by gamma-secretase processing of the p75NTR homolog NRADD. Journal of cell science. 117(Pt 18): 4099-111.
    [4] De Smedt, Magda., et al., 2005. Different thresholds of Notch signaling bias human precursor cells toward B-, NK-, monocytic/dendritic-, or T-cell lineage in thymus microenvironment. Blood. 106(10): 3498-506.
    [5] El Mouedden, Mohammed., et al., 2006. Reduction of Abeta levels in the Sprague Dawley rat after oral administration of the functional gamma-secretase inhibitor, DAPT: a novel non-transgenic model for Abeta production inhibitors. Current pharmaceutical design. 12(6): 671-6. PMID: 16472156

    分子式
    C23H26F2N2O4    		 分子量
    432.46    		 CAS号
    208255-80-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >70 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    50 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01459627 Myocardial Infarction|Cardiovascular Disease Other: 6 months DAPT|Other: 12 months DAPT Maasstad Hospital|Medtronic Phase 4 2011-12-01 2016-12-02
    NCT01106534 Chronic Total Occlusion of Coronary Artery|Vascular Disease|Myocardial Ischemia|Coronary Artery Stenosis|Coronary Disease|Coronary Artery Disease|Coronary Restenosis Drug: placebo + aspirin|Drug: clopidogrel + aspirin OR prasugrel + aspirin|Device: XIENCE V Everolimus Eluting Coronary Stent System (XIENCE V EECSS) Abbott Vascular|Baim Institute for Clinical Research|Bristol-Myers Squibb|Eli Lilly and Company|Daiichi Sankyo Inc. Phase 4 2009-08-01 2016-05-12
    NCT01325935 Coronary Artery Disease Drug: Clopidogrel Associations for Establishment of Evidence in Interventions|Medtronic Phase 4 2011-04-01 2016-01-05
    NCT02605447 Coronary Artery Disease Drug: 3 months of dual antiplatelet therapy (DAPT)|Device: SYNERGY Stent System Boston Scientific Corporation Phase 4 2016-01-01 2017-03-02
    NCT02609698 Stable Angina, Unstable Angina, Silent Coronary Ischemia, Coronary Artery Disease Device: Coroflex ISAR|Drug: 3 months DAPT|Drug: 6 months DAPT Ajou University School of Medicine|B. Braun Korea Co., Ltd. Phase 4 2015-08-01 2015-11-18
    NCT03023020 High Bleeding Risk|Coronary Artery Disease|PCI Drug: Aspirin|Drug: P2Y12 inhibitor|Drug: Clopidogrel ECRI bv|Cardialysis B.V.|European Cardiovascular Research Center|University of Bern|Terumo Medical Corporation 2017-02-01 2017-01-13
    NCT03008083 Drug-Eluting Stents|Percutaneous Coronary Intervention Drug: 3 months DAPT|Drug: 12 months DAPT Shanghai MicroPort Medical (Group) Co., Ltd. Phase 4 2017-07-01 2016-12-30
    NCT02798913 Peripheral Artery Disease Drug: Short DAPT|Drug: Long DAPT Federico II University Phase 3 2016-01-01 2016-08-11
    NCT02118870 Acute Coronary Syndrome Drug: Treatment 90 days DAPT|Drug: Treatment 360 days DAPT Diagram B.V. Phase 4 2014-04-01 2016-08-01
    NCT02619760 Coronary Artery Disease Drug: 1-month DAPT|Drug: 12-month DAPT Kyoto University, Graduate School of Medicine Phase 4 2015-12-01 2016-07-11
    NCT00963781 Coronary Artery Disease|Coronary Thrombosis Device: Medtronic Endeavor Stent|Drug: Reduced duration (6 months) DAPT Scripps Health|Medtronic Phase 4 2009-08-01 2012-12-20
    NCT00977938 Coronary Artery Disease Drug: Placebo & Aspirin|Drug: Clopidogrel & Aspirin, Prasugrel & Aspirin Baim Institute for Clinical Research|Abbott|Boston Scientific Corporation|Bristol-Myers Squibb|Sanofi-Synthelabo|Cordis Corporation|Eli Lilly and Company|Daiichi Sankyo Inc.|Medtronic Phase 4 2009-10-01 2015-09-18
    NCT00954707 Coronary Artery Disease Drug: Clopidogrel & Aspirin, Prasugrel & Aspirin|Drug: Placebo & Aspirin Cordis Corporation Phase 4 2009-08-01 2014-01-13
    NCT02513810 Coronary Artery Disease Device: BioFreedom with 1 month DAPT|Device: BioMatrix Flex with 6 to 12 months DAPT Yonsei University 2015-07-01 2016-09-05
    NCT01514227 Coronary Artery Disease Drug: Aspirin or thienopyridine|Drug: Aspirin and thienopyridine Associations for Establishment of Evidence in Interventions Phase 4 2011-12-01 2017-01-26
    NCT02601157 Stable Angina|Unstable Angina|Non-ST Segment Elevation Myocardial Infarction Device: CX-ISAR|Device: Orsiro|Drug: 3-months DAPT|Drug: 1-year DAPT Seoul National University Hospital|B. Braun Korea Co., Ltd. Phase 4 2015-12-01 2017-02-24
    NCT02303717 Coronary Artery Disease Device: Percutaneous coronary intervention|Drug: Dual antiplatelet therapy NHS National Waiting Times Centre Board|Boston Scientific Corporation|Venn Life Sciences|Cardialysis B.V.|Diagram B.V. 2014-12-01 2014-11-25
    NCT02808039 Dual Antiplatelet Therapy|Platelet Reactivity Other: Platelet reactivity testing Rabin Medical Center 2016-09-01 2016-06-17

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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