| 中文名称: | LY404039 | ||||
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| 英文名称: | LY404039 | ||||
| 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;(1R,4S,5S,6S)-4-氨基-2-硫杂双环[3.1.0]己烷-4,6-二甲酸 2,2-;LY404039 抑制剂;LY404039 国华试剂 (1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide；Pomaglumetad | ||||
| CAS No: | 635318-11-5 | 分子式: | C7H9NO6S | 分子量: | 235.21 |
| CAS No: | 635318-11-5 | ||||
| 分子式: | C7H9NO6S | ||||
| 分子量: | 235.21 | ||||
基本信息
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产品编号： |
L11027 |
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产品名称： |
LY404039 |
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CAS: |
635318-11-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
235.21 |
-20℃ |
1个月 |
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化学名： |
(1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
4.2515mL |
21.2576mL |
42.5152mL |
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5mM |
0.8503mL |
4.2515mL |
8.5030mL |
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10mM |
0.4252mL |
2.1258mL |
4.2515mL |
生物活性
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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。 |
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靶点 |
mGlu2 Receptor 149nM (Ki,Recombinant human mGluR2) |
hmGluR3 92nM (Ki) |
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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. |
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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. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
