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LDN 212320
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LDN 212320图片
CAS NO:894002-50-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
LDN 212320 (LDN-0212320) 是一种谷氨酸转运蛋白 (GLT-1)/兴奋性氨基酸转运蛋白 2 (EAAT2) 激活剂(在翻译水平)。
Cas No.894002-50-7
别名LDN-0212320; OSU-0212320
化学名3-((2-methylbenzyl)thio)-6-(pyridin-2-yl)pyridazine
Canonical SMILESCC1=CC=CC=C1CSC2=NN=C(C3=CC=CC=N3)C=C2
分子式C17H15N3S
分子量293.39
溶解度DMSO: 25 mg/mL,Ethanol: 5 mg/mL
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by >6 fold at concentrations< 5 μM after 24 h.IC50 value: 1.83 uM(EC50) [2]Target: EAAT2 activatorin vitro: LDN/OSU-0212320 increased EAAT2 protein levels in a dose-dependent(EC50=1.83 ± 0.27 μM) and time-dependent manner. LDN/OSU-0212320 increased EAAT2 protein levels and glutamate uptake function, but did not affect EAAT1 or EAAT3 protein levels. LDN/OSU-0212320 treatment markedly prevented neuronal loss and degeneration, as assessed by MAP2 immunostaining [2]. in vivo: After a single i.p. 40-mg/kg dose of LDN/OSU-0212320, 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). In addition, we found that LDN/OSU-0212320–induced EAAT2 protein levels and glutamate uptake were dose dependent [2].Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotectionBy Kong, Qiongman; Chang, Ling-Chu; Takahashi, Kou; Liu, Qibing; Schulte, Delanie A.; Lai, Liching; Ibabao, Brian; Lin, Yuchen; Stouffer, Nathan; Das Mukhopadhyay, Chitra; et alFrom Journal of Clinical Investigation (2014), 124(3), 1255-1267. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activatorsBy Xing, Xuechao; Chang, Ling-Chu; Kong, Qiongman; Colton, Craig K.; Lai, Liching; Glicksman, Marcie A.; Lin, Chien-Liang Glenn; Cuny, Gregory D. From Bioorganic & Medicinal Chemistry Letters (2011), 21(19), 5774-5777.

References:
[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.