MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
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 | Decoglurant | VU6010572 | FPTQ | (S)-MCPG | L-Glutamine-d5 | Mavoglurant racemate | L-Glutamine-13C5,15N2 | DFMTI | VU0360172 | JNJ16259685 | FITM | VU0483605 | LSN2463359 | mGlu4 receptor agonist 1 | LSP4-2022 | AMN082 | JF-NP-26 | Xanthurenic acid-d4 | Talaglumetad hydrochloride | ABP688 | Fasoracetam | Kainic acid hydrate | VU 0364439 | mGluR2 antagonist 1 | 3,3'-Difluorobenzaldazine | trans-ACPD | VU 0357121 | PHCCC | DCG-IV | TCN238
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。