DAPT

  Cat. No.:  DC7396   Featured
Chemical Structure
208255-80-5
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More than 5000 active chemicals with high quality for research!
Field of application
DAPT(GSI-IX) is an inhibitor of γ-secretase; DAPT causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ and Aβ42 respectively) and in brain extract, cerebrospinal fluid and plasma.
Cas No.: 208255-80-5
Chemical Name: Dapt
Synonyms: DAPT;Glycine, N-[(3,5-difluorophenyl)acetyl]-L-alanyl-2-phenyl-,1,1-dimethylethyl ester, (2S)-;((S)-tert-butyl 2-((S)-2-(2-(3,5-difluorophenyl)acetamido)propanamido)-2-phenylacetate);(S)-tert-Butyl 2-((S)-2-(2-(3,5-difluorophenyl)acetamido)propanamido)-2-phenylacetate;DAPT DAPT;DAPT (GSI-IX);DAPT (GSI-IX, LY-374973);N-[(3,5-Difluorophenyl)acetyl]-L-alanyl-2-phenyl]glycine-1,1-dimethylethyl ester(DAPT);N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester;tert-butyl (2S)-2-[[(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]propanoyl]amino]-2-phenylacetate;(3,5-Difluorophenylacetyl)-Ala-Phg-OtBu;(3,5-Difluorophenylacetyl)-L-alanyl-L-2-phenylglycine tert-Butyl Ester;GSI IX;GSI-IX;GSI-IX LY-374973 N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester;N-[N-(3,5-difluorophenylacetyl)-L-alanyl]-(S)-phenylglycine t-butyl ester;LY-374973;DAPT (enzyme inhibitor);(2S)-N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-2-phenylglycine tert-butyl ester;gamma-Secretase Inhibitor IX;InSolution™ gamma-Secretase Inhibitor IX;N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester;GSIIX;PubChem22
SMILES: FC1C([H])=C(C([H])=C(C=1[H])C([H])([H])C(N([H])[C@@]([H])(C([H])([H])[H])C(N([H])[C@]([H])(C(=O)OC(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)=O)F
Formula: C23H26F2N2O4
M.Wt: 432.4604
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: DAPT is a γ-secretase inhibitor with IC50s of 115 and 200 nM for total Aβ and Aβ42, respectively.
In Vivo: DAPT is administered to PDAPP mice (100 mg/kg s.c.) and the levels of DAPT and Aβ are examined in the brain cortex. Peak DAPT levels of 490 ng/g are achieved in the brain 3 h after treatment, and levels greater than 100 ng/g (~200 nM) are sustained throughout the first 18 h. These brain concentrations of DAPT are in excess of its IC50 for lowering Aβ in neuronal cultures (115 nM), and results in a robust and sustains pharmacodynamic effect[1]. DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and Nuclear factor kappa B in rats. Western blot analyses also show a significant decrease of Notch 1 and NF-κB expression in DAPT (0.03 mg/kg) group (P<0.05 vs. MCAO group)[3].
In Vitro: DAPT inhibits Aβ production over 90%, effects only a modest reduction in APPβ in the culture media. Although APPβ is reduced by about 30% by DAPT treatment, this effect is not concentration-dependent and is reversed by the removal of DAPT[1]. CNE-2 cells are treated with increasing concentrations of DAPT (0, 25, 50 and 75 μM), and the γ-secretase-generated Notch 1 fragment Val1744-NICD is decreased after 48 h in a dose-dependent manner (P<0.01). The activation of γ-secretase is almost completely inhibited by DAPT at the concentration of 50 μM[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC48365 RO7185876 RO7185876 is a potent and selective gamma secretase modulator as a potential treatment for Alzheimer's disease.
DC47320 FRM-024 FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.
DC7666 MK0752 MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
DC8215 RO4929097 RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
DC10926 LY900009 LY900009 (LY-900009) is an orally active small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.
DC5036 LY-411575 LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.
DC8615 L-685,458 L-685,458 is a selective and Potent inhibitor of γ-secretase with IC50 value of 17 nM.
DC8277 E-2012 E 2012 is a potent γ-secretase modulator.
DC7396 DAPT DAPT(GSI-IX) is an inhibitor of γ-secretase; DAPT causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ and Aβ42 respectively) and in brain extract, cerebrospinal fluid and plasma.
DC3114 Avagacestat (BMS-708163) BMS-708163 is a potent, selective γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, respectively.
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