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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.58%
- 分子式: C41H49F3N2O8
- 分子量:754.83
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
製品説明
体外実験
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.
体内実験
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.
化学情報
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性状 Oil
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分子量 754.83
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)