DAPT CAS: 208255-80-5
DAPT is a potent and specific inhibitor of γ-secretase.

DAPT (CAS 208255-80-5)

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备用名: Gamma-Secretase Inhibitor IX;N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-butyl ester
应用; DAPT is a potent and specific inhibitor of γ-secretase
CAS号码: 208255-80-5
纯度: ≥95%
分子量: 432.46
分子式: C23H26F2N2O4
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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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).


参考文献

1. Dovey, H F., et al., 2001. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. Journal of neurochemistry. 76(1): 173-81. PMID: 11145990

2. Geling, Andrea., et al., 2002. A gamma-secretase inhibitor blocks Notch signaling in vivo and causes a severe neurogenic phenotype in zebrafish. EMBO reports. 3(7): 688-94. PMID: 12101103

3. 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. PMID: 12626636

4. 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. PMID: 15280425

5. 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. PMID: 16030192

6. 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

用法 :
DAPT is soluble in DMSO.
外观 :
Powder
物理状态 :
Solid
溶解度 :
Soluble in DMSO (15 mg/mL), ethanol (~1 mg/mL), dichloromethane, DMF (~25 mg/mL), and 1:9 solution of DMF:PBS(pH 7.2) (~0.1 mg/mL).
保存 :
Store at -20° C
沸点 :
~612.2° C at 760 mmHg (Predicted)
密度 :
~1.2 g/cm3 (Predicted)
折射率 :
n20D 1.53 (Predicted)
IC50 :
total Aβ: IC50 = 115 nM (human); Aβ42: IC50 = 200 nM (human)
pK值 :
pKa: 12.82 (Predicted)
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
PubChem CID :
MDL 号码 :
MFCD04974585
SMILES :
C[[email protected]@H](C(=O)N[[email protected]@H](C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F

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PMID: # 33781742  Wang, J.|Yan, X.|Feng, W.|Wang, Q.|Shi, W.|Chai, L.|Zhang, Q.|Chen, Y.|Liu, J.|Qu, Z.|Xie, X.|Li, M.| et al. 2021. J Biol Chem. 100599.

PMID: # 30951821  Bruno, A. et al. 2019. Biochim Biophys Acta Mol Basis Dis. 1865: 1642-1650.

PMID: # 30839137  Niu, Y. et al. 2019. Cell Biol. Int.

PMID: # 29393429  Chen, DW. et al. 2018. Mol Med Rep. 17: 4965-4972.

PMID: # 29636838  Yu, L. et al. 2018. Oxid Med Cell Longev. 2018: 2750695.

PMID: # 29345284  Li, L. et al. 2018. Int. J. Oncol. 52: 473-484.

PMID: # 29286081  Liu, Z. et al. 2018. Int. J. Mol. Med. 41: 1560-1572.

PMID: # 28771710  Lee, ML. et al. 2017. J. Neurochem.

PMID: # 27901069  Mariscal, J. et al. 2016. Sci Rep. 6: 37820.

PMID: # 26523864  Zhao, E. et al. 2016. Nat. Immunol. 17: 95-103.

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