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DAPT (GSI-IX) 目录号 GC12942

γ-secretase inhibitor,potent and specific

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥452.00
现货
10mg
¥504.00
现货
50mg
¥1,974.00
现货
500mg
¥7,613.00
现货

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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

SHG -44 human glioma cell line

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

5d; 1.0 μM

Applications

Cell viability in each group was detected by MTT. Compared with those in group A (control), proliferation of SHG -44 cells in group B (0.5 μM), C (1μM), D (5 μM) and E (10 μM) were inhibited by DAPT. For group B and A, the results were significantly different (P<0.05). However, cell viability of group B was significantly higher than those in group C, D and E (P<0.05). The results showed that increased inhibition effect was related to increased DAPT concentrations. However there was no difference among group C, D and E (P>0.05). It indicated that DAPT is a concentration-dependent inhibitor that may obviously inhibit SHG-44 cells proliferation. As concentration of DAPT higher than 1.0 μmol/L showed no more obvious disparities in cell inhibition, concentration of 1.0 μmol/L was our prioriy.

Animal experiment [2]:

Animal models

Male Balb/C mice

Dosage form

10 mg/kg/day; subcutaneously injected

Applications

CT26 colon adenocarcinoma cells (5 × 105 cells) in 500 μL of Phosphate buffer solution (PBS) were inoculated subcutaneously into the dorsum of all mice. Administration of DAPT significantly reduced serum sVEGFR1, while could not change serum VEGF concentration in control mice. Immunohistochemical study of the tumors showed that CD31 positive cells were reduced after DAPT administration (280.6 ± 81 vs. 386 ± 59.9 CD31 positive cells/mm2), although it was not statistically significant.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Liu X, Xu Q R, Xie W F, et al. DAPT suppresses the proliferation of human glioma cell line SHG-44[J]. Asian Pacific journal of tropical medicine, 2014, 7(7): 552-556.

[2] Kalantari E, Saeidi H, Kia N S, et al. Effect of DAPT, a gamma secretase inhibitor, on tumor angiogenesis in control mice[J]. Advanced biomedical research, 2013, 2.

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Chemical Properties

Cas No. 208255-80-5 SDF
别名 gamma-Secretase Inhibitor IX, DAPT, GSI-IX
化学名 tert-butyl (2S)-2-[[(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanoyl]amino]-2-phenylacetate
Canonical SMILES CC(C(=O)NC(C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F
分子式 C23H26F2N2O4 分子量 432.46
溶解度 ≥ 21.623mg/mL in DMSO, ≥ 16.36 mg/mL in EtOH with ultrasonic 储存条件 Store at 4°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

DAPT, N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester, is a potent and specific inhibitor of  γ-secretase, a multimeric membrane protein complex that catalyzes proteolytic cleavage of amyloid precursor protein (APP) resulting in the accumulation of amyloi-β (Aβ) peptides which is associated with early on-set of familial Alzheimer’s disease (AD). It directly binds to the C-terminal fragment of the catalytic center of γ-secretase, presenilin (PS), especially within the transmenbrane domain 7 or more C-terminal region, resulting in the synthesis of a photoactivable DAPT derivative. Through oral administration, DAPT  dose-dependently reduced Aβ peptides levels in vivo in Plasma and cerebrospinal fluid in young (6 months old, plaque-free) and aged (17 months old, plaque-bearing) Tg2576 mice.

Reference

[1].Thomas A. Lanz, Carol S. Himes, Giovanni Pallante, Lisa Adams, Shinji Yamazaki, Ben Amore, and Kalpana M. Merchant. The γ-secretase inhibitor N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester reduces Aβ levels in vivo in plasma and cerebrospinal fluid in young (plague-free) and aged (plaque-bearing) Tg2576 mice. The Journal of Pharmacology and Experimental Therapeutics 2003: 305 (3) 864-871
[2].Yuichi Morohashi, Toshiyuki Kan, Yusuke Tominari, Haruhiko Fuwa, Yumiko Okamura, Naoto Watanabe, Chihiro Sato, Hideaki Natsugari, Tohru Fukuyama, Takeshi Iwatsubo, and Taisuke Tomita. C-terminal fragment of presenilin is the molecular target of a dipeptidic γ-secretase-specific inhibitor DAPT (N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl Ester). The Journal of Biological Chemistry 2006: 281(21) 14670-14676