PBA-1105 TFA
PBA-1105 TFA is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 TFA selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 TFA increases the autophagic flux of Ub-conjugated aggregates.
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- Pureza : 99.58%
- Fòrmula: C41H49F3N2O8
- Peso molecular:754.83
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
PBA-1105 TFA induces autophagic degradation of stably expressed mutant tau at DC50 of 0.71 nM and Dmax,24 hr of 100 nM, followed by a hook effect at higher concentrations[1].
PBA-1105 (0.1-10 μM; 24 hours) TFA induces the autophagic degradation of misfolded proteins and aggregates at nanomolar concentrations. PBA-1105 TFA leads to significant degradation of mutant tau and misfolded proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:1 μM
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Incubation Time:24 hours
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Result:Activated p62 oligomerization and increased autophagic flux of ubiquitinated aggregates.
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Cell Line:SH-SY5Y-tauP301L cells
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:24 hours
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Result:Selectively degraded mutant tauP301L with a DC50 of 0.71 nM and persistently cleared insoluble tau aggregates.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:hTauP301L-BiFC transgenic mice[1]
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Dosage:20 mg/kg or 50 mg/kg (PBS containing 30% polyethylene glycol (PEG))
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Administration:Intraperitoneal injection; three times per week; for 4 weeks
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Result:Effectively cleared tau aggregates in a dose-dependent manner, significantly reducing insoluble tau species in the brain while leaving soluble tau species unaffected.
Resulted in increased levels of autophagic markers like LC3, confirming the activation of autophagic degradation pathways.
Immunohistochemical analysis showed a marked reduction in tau oligomers and phosphorylated tau in both cortical and hippocampal regions.
Chemical Information
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Appearance Oil
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Peso molecular 754.83
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Fòrmula C41H49F3N2O8
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Color Colorless to light yellow
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SMILES
O=C(O)C(F)(F)F.O=C(CCCC1=CC=CC=C1)NCCOCCOCCOCCNCC2=CC(OCC3=CC=CC=C3)=C(OCC4=CC=CC=C4)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
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Ficha de datos (268 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PBA-1105 TFA Related Classifications
HY-161743A Related Classifications
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