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LDN-212320

CAS号

894002-50-7

分子式

C17H15N3S

主要靶点

transporter

仅限科研使用

Cat No : CM11325

Print datasheet

Synonyms

LDN 0212320|LDN/OSU 0212320|LDN/OSU0212320|LDN/OSU-0212320|LDN 212320|LDN212320|LDN-212320|LDN0212320|LDN-0212320|OSU 0212320|OSU0212320|OSU-0212320|Excitatory amino acid transporter 2|Glutamate transporter 1|GLT-1|EAAT2

验证数据展示

  • CAS No.: 894002-50-7

    LDN-212320
    CAS#: 894002-50-7

产品信息

CAS号 894002-50-7
分子式 C17H15N3S
主要靶点 transporter
主要通路 代谢
分子量 293.39
纯度 98.13%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 LDN 0212320|LDN/OSU 0212320|LDN/OSU0212320|LDN/OSU-0212320|LDN 212320|LDN212320|LDN-212320|LDN0212320|LDN-0212320|OSU 0212320|OSU0212320|OSU-0212320|Excitatory amino acid transporter 2|Glutamate transporter 1|GLT-1|EAAT2

体内活性

After LDN/OSU-0212320(a single i.p.; 40-mg/kg) treatment, EAAT2 protein levels and associated glutamate uptake increased by approximately 1.5- to 2-fold at 2 hours and by approximately 2- to 3-fold between 8 and 24 hours after injection. Even 72 hours after injection, an approximately 1.5-fold increase in EAAT2 protein levels could still be detected (data not shown). LDN/OSU-0212320–induced EAAT2 protein levels and glutamate uptake was dose-dependent [2].

体外活性

LDN/OSU-0212320 enhanced EAAT2 protein levels and glutamate uptake function but did not affect EAAT1 or EAAT3 protein levels and it also increased EAAT2 protein levels in a dose-dependent (EC50: 1.83 ± 0.27 μM) and time-dependent manner. LDN/OSU-0212320 treatment markedly prevented neuronal loss and degeneration, as assessed by MAP2 immunostaining [2].

溶解度

DMSO:16.67 mg/mL (56.81 mM)

参考文献

1.Xing X, et al. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5774-7.
2.Kong Q, et al. Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotection. J Clin Invest. 2014 Mar;124(3):1255-67.

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