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- 保存条件：
Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
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MedChemExpress LLC
- CAS号：
635318-11-5
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥550.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥500.0 |
| 规格： | 10 mg | 产品价格： | ￥900.0 |
| 规格： | 25 mg | 产品价格： | ￥2000.0 |
| 规格： | 50 mg | 产品价格： | ￥3500.0 |
| 规格： | 100 mg | 产品价格： | ￥6100.0 |
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LY404039
CAS No. : 635318-11-5
MCE 国际站：LY404039
产品活性：LY404039 是一种有效的，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 149 nM 和 92 nM，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。
研究领域：GPCR/G Protein | Neuronal Signaling
作用靶点：mGluR
In Vitro: LY404039 is a nanomolar potent agonist in rat neurons expressing native mGlu2/3 receptors (Ki = 88 nM).
?Functionally, LY404039 potently inhibits Forskolin-stimulated cAMP formation in cells expressing human mGlu2 (EC50 = 23 nM) and mGlu3 receptors (EC50 = 48 nM).
?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 82.3 nM and with a near maximal suppression of 85.6% at 1 μM.
?LY404039 inhibits the binding of the D2-specific antagonist, [3H]domperidone, to the human cloned D2 receptor with dissociation constants of 8.2 nM at D2High and 1640 nM at D2Low. Using rat striatal tissue, LY404039 has dissociation constants of 12.6 nM at D2High and 2100 nM at D2Low.
In Vivo: LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion (3-30 and 10 mg/kg, respectively). LY404039 (3-10 mg/kg) inhibits conditioned avoidance responding. LY404039 also reduces fear-potentiated startle in rats (3-30 μg/kg) and marble burying in mice (3-10 mg/kg), indicating anxiolytic-like effects. LY404039 (10 mg/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 10 mg/kg, exposure increased proportionally with dose. LY404039 (10 mg/kg; p.o.) treatment shows the Cmax is 1528.5 ng/mL and Tmax is 2 hours in rats.
相关产品：Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | Orally Active Compound Library | Neurotransmitter Receptor Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | L-Glutamine | LY341495 | Ro 67-7476 | Xanthurenic acid | DHPG | Eglumegad | MPEP Hydrochloride | MTEP hydrochloride | CHPG sodium salt | CTEP | JNJ16259685 | (RS)-MCPG | LY2794193 | LY367385 hydrochloride | O-Phospho-L-serine | Mavoglurant | Dipraglurant | NPS 2390 | MMPIP hydrochloride | MSOP | RO0711401 | AMN082 | Basimglurant | Foliglurax monohydrochloride | JNJ-40411813 | VU0650786
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文献和实验刘淼清 在园中看到关于LY294002和Wortmannin区别。（建议用LY，主要原因有两个，一，Wortmannin相对来说要贵好多；二，更重要的，Wortmannin半衰期很短，如果没记错的话大概只有8－10小时，所以如果处理时间久的话，药物浓度下降很快。有篇文献研究了Wortmannin的半衰期，有兴趣可以去查查看，应该是2005年的文献。 ） 这篇文献不知有哪位战友知道。 第二 LY294002的半衰期是多少
olivial 最近在做细胞内信号转导通路PI-3K-Akt，关于它的抑制剂LY 294002的配制，说明书上写用DMSO，在做实验时设了vehicle（含等量DMSO）组，但发现DMSO对细胞（小胶质细胞）有影响，且DMSO与干预药有协同作用，MTT结果显示DMSO浓度>=0.1%即对细胞造成损伤，而任何浓度DMSO（0.01%~0.1%）都与干预药有协同作用，乙醇的结果亦如此。所以想请教，大家在配LY时是怎么配的？在使用LY时是否遇到了上述问题
Determining Ligand Specificity of Ly49 Receptors
Ly49 receptors in rodents, like KIR in humans, play an integral role in the regulation of NK cell activity. Some inhibitory Ly49 are known to interact with specific MHC I alleles to maintain tolerance to self tissues, and NK activation
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