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LY404039  ≥98%

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溶解性：溶于水(5mg/mL超声并用水调整ph值到8）
产品描述：基本信息 产品编号： L11027 产品名称： LY404039 CAS: 635318-11-5   储存条件 粉末 -20℃ 四年 分子式： C7H9NO6S 溶于液体 -80℃ 6个月 分子量： 235.21 -20℃ 1个月 化学名：  (1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 4.2515mL 21.2576mL 42.5152mL 5mM 0.8503mL 4.2515mL 8.5030mL 10mM 0.4252mL 2.1258mL 4.2515mL   生物活性 产品描述 一种有效的，选择性的，具有口服活性的 mGluR2 和 mGluR3 激动剂，对重组人 mGluR2 和 mGluR3 的 Ki 分别为 149nM 和 92nM，比对其他受体/转运蛋白的抑制性高 100 倍以上。LY404039 具有抗精神病和抗焦虑的作用。 靶点 mGlu2 Receptor 149nM (Ki,Recombinant human mGluR2) hmGluR3 92nM (Ki)   体外研究 LY404039 is a nanomolar potent agonist in rat neurons expressing native mGlu2/3 receptors (Ki=88nM).Functionally,LY404039 potently inhibits Forskolin-stimulated cAMP formation in cells expressing human mGlu2 (EC50=23nM) and mGlu3 receptors (EC50 =48nM).Electrophysiological studies indicate that LY404039 suppresses electrically evoked excitatory activity in the striatum,and serotonin-induced L-glutamate release in the prefrontal cortex.LY404039 suppresses the frequency of 5-HT-induced excitatory postsynaptic currents (EPSCs) with an EC50 of 82.3nM and with a near maximal suppression of 85.6% at 1μM.LY404039 inhibits the binding of the D2-specific antagonist,[3H]domperidone,to the human cloned D2 receptor with dissociation constants of 8.2nM at D2High and 1640nM at D2Low.Using rat striatal tissue,LY404039 has dissociation constants of 12.6nM at D2High and 2100nM at D2Low. 体内研究 LY404039 attenuates amphetamine-and phencyclidine-induced hyperlocomotion (3-30 and 10mg/kg,respectively).LY404039 (3-10mg/kg) inhibits conditioned avoidance responding.LY404039 also reduces fear-potentiated startle in rats (3-30μg/kg) and marble burying in mice (3-10mg/kg),indicating anxiolytic-like effects.LY404039 (10mg/kg) also increases dopamine and serotonin release/turnover in the prefrontal cortex.Following oral administration of LY404039 to fasted rats at doses of 1,3,or 10mg/kg,exposure increased proportionally with dose.LY404039 (10mg/kg;p.o.) treatment shows the Cmax is 1528.5ng/mL and Tmax is 2 hours in rats.
保存条件：-20℃

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