LDN-212320

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LDN-212320 是一种谷氨酸转运蛋白 EAAT2 激活剂。 24 小时后，浓度 < 5 μM 时，它还能将 EAAT2 水平提高 6 倍以上。

LDN-212320 is a glutamate transporter EAAT2 activator. It also enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.(In Vitro):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 .(In Vivo):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 .

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LDN-212320 (10 or 20 mg/kg, i.p) significantly attenuates formalin-evoked nociceptive behavior. LDN-212320 (10 or 20 mg/kg, i.p) significantly reverses formalin-induced impaired hippocampal-dependent behavior. In addition, LDN-212320 (10 or 20 mg/kg, i.p) increases GLT-1 expressions in the hippocampus and ACC.LDN-212320 (20 mg/kg, i.p) significantly reduced formalin induced-ERK phosphorylation, a marker of nociception, in the hippocampus and ACC. Animal Model:Mice.Dosage:10 or 20 mg/kg.Administration:IP 24 h before the injection of formalin.Result:Significantly attenuated licking and biting behavior during both phases 1 and 2 in a dose-dependent manner compared to formalin-injected mice.Significantly (P < 0.01 or P < 0.001) reduced the licking and biting behavior.Significantly increased preference for the displaced object (F3, 13 = 28.03, P < 0.01) compared to formalin-injected mice.Significantly (P < 0.001) increased interaction time with the displaced object compared to formalin-injected mice.

LDN/OSU-0212320 | LDN-0212320 | OSU-0212320

Others

Other Targets

NK2

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894002-50-7

293.39

C17H15N3S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (170.42 mM)

Cc1ccccc1CSc1ccc(nn1)-c1ccccn1

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(-20℃)

With Ice Pack

≥ 2 years