1. Neuronal Signaling
  2. α-synuclein
  3. PBT434 mesylate

PBT434 mesylate  (Synonyms: ATH434 mesylate)

目录号: HY-120475A 纯度: 99.74%
COA 产品使用指南

PBT434 methanesulfonate 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 methanesulfonate 可作为铁螯合剂和调节跨细胞铁运输。PBT434 methanesulfonate 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 methanesulfonate 可防止黑质致密部神经元 (SNpc) 丢失。PBT434 methanesulfonate 具有用于帕金森病 (PD) 研究的潜力。

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PBT434 mesylate Chemical Structure

PBT434 mesylate Chemical Structure

CAS No. : 2387898-69-1

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5 mg ¥9500
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Other Forms of PBT434 mesylate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PBT434 methanesulfonate is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 methanesulfonate can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 methanesulfonate inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 methanesulfonate prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 methanesulfonate has the potential for the research of Parkinson’s disease (PD)[1][2].

体外研究
(In Vitro)

PBT434 methanesulfonate (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 methanesulfonate (0-100 µM; 24 h) 对脑微血管内皮细胞没有细胞毒性作用[2]
PBT434 methanesulfonate (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.

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 methanesulfonate (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 (MPTP 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

398.26

Formula

C13H17Cl2N3O5S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (251.09 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5109 mL 12.5546 mL 25.1092 mL
5 mM 0.5022 mL 2.5109 mL 5.0218 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.74%

参考文献

PBT434 mesylate 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5109 mL 12.5546 mL 25.1092 mL 62.7731 mL
5 mM 0.5022 mL 2.5109 mL 5.0218 mL 12.5546 mL
10 mM 0.2511 mL 1.2555 mL 2.5109 mL 6.2773 mL
15 mM 0.1674 mL 0.8370 mL 1.6739 mL 4.1849 mL
20 mM 0.1255 mL 0.6277 mL 1.2555 mL 3.1387 mL
25 mM 0.1004 mL 0.5022 mL 1.0044 mL 2.5109 mL
30 mM 0.0837 mL 0.4185 mL 0.8370 mL 2.0924 mL
40 mM 0.0628 mL 0.3139 mL 0.6277 mL 1.5693 mL
50 mM 0.0502 mL 0.2511 mL 0.5022 mL 1.2555 mL
60 mM 0.0418 mL 0.2092 mL 0.4185 mL 1.0462 mL
80 mM 0.0314 mL 0.1569 mL 0.3139 mL 0.7847 mL
100 mM 0.0251 mL 0.1255 mL 0.2511 mL 0.6277 mL
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.

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产品名称:
PBT434 mesylate
目录号:
HY-120475A
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