DAPTCAS: 208255-80-5
MF: C23H26F2N2O4
MW: 432.46
A potent and specific inhibitor of γ-secretase.

DAPT (CAS 208255-80-5)

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Sinónimo: Gamma-Secretase Inhibitor IX;N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-butyl ester
Solicitud: A potent and specific inhibitor of γ-secretase
Número de CAS: 208255-80-5
Pureza: ≥95%
Peso Molecular: 432.46
Fórmula Molecular: C23H26F2N2O4
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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).


References

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

Uso :
DAPT is soluble in DMSO.
Apariencia :
Powder
Estado de Materia :
Solid
Solubilidad :
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).
ALMACENAMIENTO :
Store at -20° C
Punto de ebullición :
~612.2° C at 760 mmHg (Predicted)
Densidad :
~1.2 g/cm3 (Predicted)
Indice de Refracción :
n20D 1.53 (Predicted)
IC50 :
total Aβ: IC50 = 115 nM (human); Aβ42: IC50 = 200 nM (human)
Valores de pK :
pKa: 12.82 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
5311272
Número MDL :
MFCD04974585
SMILES :
C[C@@H](C(=O)N[C@@H](C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F

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DAPT  Menciones del Producto

Ver como otros han utilizado DAPT. Haga click en la entrada de PubMed .

Citaciones 1 a 10 de un total de 29

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

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

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

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

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

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

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

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

PMID: # 26648098  Gao, Y. et al. 2016. International journal of oncology. 48: 281-92.

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

Citaciones 1 a 10 de un total de 29
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