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编 号:F751930
分子式:C13H17Cl2N3O5S
分子量:398.26
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1mg
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5mg
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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).

体内研究:
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]。Animal Model:12 weeks, 25 g, Male C57BL/6 J mice (6-OHDA intoxication model)
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)
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.

体外研究:
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。PBT434 methanesulfonate (0-100 μM; 24 h) 对脑微血管内皮细胞没有细胞毒性作用。PBT434 methanesulfonate (20 μM; 24 h) 增加 hBMVEC 中总 TfR、Cp 蛋白水平的表达。
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