1. PROTAC Autophagy
  2. AUTOTACs Autophagy
  3. PBA-1105 TFA

PBA-1105 TFA 是一种自噬靶向嵌合体 (AUTOTAC),可诱导 p62 自我寡聚化。PBA-1105 TFA 选择性地与错误折叠蛋白质的暴露疏水区域结合,通过自噬 (autophagy) 途径促进其降解。PBA-1105 TFA 增加了 Ub 结合聚集体的自噬通量。

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PBA-1105 TFA Chemical Structure

PBA-1105 TFA Chemical Structure

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5 mg ¥1650
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PBA-1105 TFA 的其他形式现货产品:

Other Forms of PBA-1105 TFA:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

体外研究
(In Vitro)

PBA-1105 TFA 在 DC50 为 0.71 nM 和 Dmax,24 hr 为 100 nM 时诱导稳定表达的突变 tau 的自噬降解,随后在更高浓度下产生钩状效应[1]
PBA-1105(0.1-10 μM;24 小时)TFA 在纳摩尔浓度下诱导错误折叠蛋白质和聚集体的自噬降解。PBA-1105 TFA 导致突变 tau 和错误折叠蛋白质显著降解[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Activated p62 oligomerization and increased autophagic flux of ubiquitinated aggregates.

Western Blot Analysis[1]

Cell Line: SH-SY5Y-tauP301L cells
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 hours
Result: Selectively degraded mutant tauP301L with a DC50 of 0.71 nM and persistently cleared insoluble tau aggregates.
体内研究
(In Vivo)

PBA-1105(20-50 mg/kg;腹膜内注射;每周三次;持续 4 周)TFA 成功减少了转基因小鼠 tauopathies 模型中的 tau 聚集和寡聚物种类[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: hTauP301L-BiFC transgenic mice[1]
Dosage: 20 mg/kg or 50 mg/kg (PBS containing 30% polyethylene glycol (PEG))
Administration: Intraperitoneal injection; three times per week; for 4 weeks
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.
分子量

754.83

Formula

C41H49F3N2O8

性状

油状物

颜色

Colorless to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
PBA-1105 TFA
目录号:
HY-161743A
需求量:
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