2. Neuronal Signaling
  3. α-synuclein
  4. PBT434

PBT434 是一种有效的、具有口服活性并可穿过血脑屏障的 α-突触核蛋白聚集 (α-synuclein aggregation) 抑制剂。PBT434 可作为铁螯合剂和调节跨细胞铁运输。PBT434 抑制铁介导的氧化还原活性和铁介导的 α-突触核蛋白聚集。PBT434 可防止黑质致密部神经元 (SNpc) 丢失。PBT434 具有用于帕金森病 (PD) 研究的潜力。

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PBT434 Chemical Structure

PBT434 Chemical Structure

CAS No. : 1232841-78-9

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规格 价格 是否有货
1 mg ￥3800
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5 mg ￥9500
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PBT434 的其他形式现货产品:

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PBT434 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PBT434 is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 has the potential for the research of Parkinson’s disease (PD)[1].

体外研究
(In Vitro)

PBT434 (0-20 µM；3 小时) 显着抑制铁产生的 H2O2，并显着降低 Fe 介导的 α-突触核蛋白聚集速率[1]。
PBT434 (0-100 µM; 24 h) 对脑微血管内皮细胞没有细胞毒性作用[2]。
PBT434 (20 µM; 24 h) 增加 hBMVEC 中总 TfR、Cp 蛋白水平的表达[2]。

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

PBT434 相关抗体:

Cell Cytotoxicity Assay[2]

Cell Line: hBMVEC
Concentration: 1, 10, 20, 50, 100 µM
Incubation Time: 24 h
Result: Showed no cytotoxic effects on brain microvascular endothelial cells.

Western Blot Analysis[2]

Cell Line: hBMVEC
Concentration: 20 μM
Incubation Time: 24 h
Result: Increased the expression of total TfR, Cp protein level.
体内研究
(In Vivo)

PBT434 (30 mg/kg；口服；每日一次，持续 21 天) 显着保留了 6-OHDA 毒模型中的神经元数量，并在 L-DOPA 模型中显示出明显更少的旋转，显着减少了 MPTP 模型中的 SNpc 神经元损失[ 1]。

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

Animal Model: 12 weeks, 25 g, Male C57BL/6 J mice (6-OHDA intoxication model)[1]
Dosage: 30 mg/kg
Administration: P.o.; daily for 21 days (commencing 3 days following induction of lesion)
Result: Prevented neuronal loss following 6-OHDA, preserving up to 75% of the SNpc neurons remaining (both Nissl and tyrosine hydroxylase (TH) positive neurons) after the initial phase of cell death.
Animal Model: 12 weeks, 25 g, Male C57BL/6 J mice (6-OHDA intoxication model)[1]
Dosage: 1, 3, 10, 30, 80 mg/kg
Administration: P.o.; daily for 21 days (commenced 24 h after induction of lesion)
Result: Increased the proportion of SNpc cells rescued, increased there was a trend to improved turning behavior, significantly increased varicosity abundance, prevented the decline in levels of the presynaptic marker synaptophysin (SYNP) in a dose-dependent manner.
分子量

383.07

Formula

C12H14BrCl2N3O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PBT434 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PBT4341232841-78-9ATH434PBT 434PBT-434ATH 434ATH-434α-synucleinα-Synorally activecross the blood-brain barrierSNpcironParkinson’s diseaseInhibitorinhibitorinhibit

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