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LY404039
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。
LY404039图片
CAS NO:635318-11-5
包装与价格：
包装价格(元)
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LY404039 是一种有效的、选择性的和具有口服活性的 mGluR2 和 mGluR3 激动剂，对重组人 mGluR2 和 mGluR3 的 Kis 分别为 149 nM 和 92 nM。
Cas No.635318-11-5
别名(1R,4S,5S,6S)-4-氨基-2-硫杂双环[3.1.0]己烷-4,6-二甲酸2,2-二氧化物
化学名(1R,4S,5S,6S)-4-amino-2,2-dioxo-2λ6-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid
Canonical SMILESC1C(C2C(C2S1(=O)=O)C(=O)O)(C(=O)O)N
分子式C7H9NO6S
分子量235.21
溶解度PBS (pH 7.2): 0.5 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

LY404039 is a potent and highly selective agonist of recombinant human mGlu2 and mGlu3 receptors and rat neurons expressing native mGlu2/3 receptor with Ki values of 149, 92 and 88 nM, respectively [1].

The inhibition of forskolin-stimulated cAMP formation has indicated that LY404039 was a nanomolar potent agonist of human mGlu2 (EC50 = 23 nM) and mGlu3 (EC50 = 48 nM) receptors. Additionally, LY404039 could concentration-dependently decrease Excitatory Postsynaptic Potentials (EPSPs) in rat striatal spiny neuron (EC50 = 141 nM). LY404039 has also been reported to suppress the frequency of 5-HT-induced Postsynaptic Currents (EC50 = 82.3 nM) in rat prefrontal cortical slices [1].

References:
[1] Rorick-Kehn LM1, Johnson BG, Burkey JL, Wright RA, Calligaro DO, Marek GJ, Nisenbaum ES, Catlow JT, Kingston AE, Giera DD, Herin MF, Monn JA,McKinzie DL, Schoepp DD. Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039). J Pharmacol Exp Ther. 2007 Apr;321(1):308-17. Epub 2007 Jan 4. J Pharmacol Exp Ther. 2007 Apr;321(1):308-17. Epub 2007 Jan 4.

 
 
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