LY487379
目录号: PL07113 纯度: ≥98%
CAS No. :353231-17-1
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中文名称
LY487379
中文别名
2,2,2-三氟-N-[4-(2-甲氧基苯氧基)苯基]-N-(3-吡啶基甲基)-乙磺酰胺
英文名称
LY487379
英文别名
2,2,2-Trifluoro-N-(4-(2-methoxyphenoxy)phenyl)-N-(pyridin-3-ylmethyl)ethanesulfonamide;2,2,2-trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(pyridin-3-ylmethyl)ethanesulfonamide;Ethanesulfonamide, 2,2,2-trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(3-pyridinylmethyl)-;LY 487379 HYDROCHLORIDE;2,2,2-Trifluoro-N-[4-(2-Methoxyphenoxy)phenyl]-N-(3-pyridinylMethyl)ethanesulfonaMidehydrochloride;4-MPPTS;LY487379
Cas No.
353231-17-1
分子式
C21H19N2O4F3S
分子量
452.45
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
LY487379 是一种选择性人 mGluR2 正变构调节剂 (PAM)。LY487379 增强谷氨酸刺激[35S]GTPγS 与 EC50 值分别为 1.7 μM 和 >10 μM 的 mGlu2 和 mGlu3 受体的结合。LY487379 可促进大鼠认知灵活性,促进行为抑制。LY487379 可用于精神分裂症研究。
生物活性
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [S]GTPγS binding with EC 50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research.
性状
Solid
体内研究(In Vivo)
LY487379 (intraperitoneal injection; 30 mg/kg; injected 30 min before the test) requires significantly fewer trials to criterion during the ED phase of the ASST in attentional set-shifting task in male Sprague-Dawley rats. But there has no significant drug effect during any other discrimination stage.
LY487379 hydrochloride (intraperitoneal injection; 10-30 mg/kg) induces an increase in microdialysate norepinephrine levels; the dose-effect resembled a bell-shape relationship increased. And it dose-dependently increases extracellular serotonin levels in the medial prefrontal cortex in male Sprague-Dawley rats.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Nikiforuk A, et al. Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats. J Pharmacol Exp Ther. 2010;335(3):665-673.
[2]. Schaffhauser H, et al. Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol Pharmacol. 2003;64(4):798-810.
溶解度数据
In Vitro: DMSO : 100 mg/mL (221.02 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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