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LY404039 {[allProObj[0].p_purity_real_show]}

货号：A358160 同义名： pomaglumetad

LY404039 is an inhibitor for mGluR1 (Ki=149 nM) and mGluR2 (Ki= 92 nM), which can also inhibit dopamine receptor.

LY404039 化学结构 CAS号：635318-11-5
LY404039 化学结构
CAS号：635318-11-5
LY404039 3D分子结构
CAS号：635318-11-5
LY404039 化学结构 CAS号：635318-11-5
LY404039 3D分子结构 CAS号：635318-11-5
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LY404039 纯度/质量文件 产品仅供科研

货号：A358160 标准纯度： {[allProObj[0].p_purity_real_show]}
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LY404039 生物活性

描述 LY404039 is a potent and selective mGluR2 and mGluR3 agonist with dissociation constants (Kis) of 149 nM for mGluR2 and 92 nM for mGluR3 in recombinant human receptors, exhibiting over 100-fold selectivity for these receptors over other receptors and transporters. LY404039 has demonstrated both antipsychotic and anxiolytic effects[1].

LY404039 动物研究

Animal study LY404039 also mitigates amphetamine- and phencyclidine-induced hyperlocomotion at doses of 3-30 mg/kg and 10 mg/kg, respectively. At doses ranging from 3 to 10 mg/kg, it inhibits conditioned avoidance responding and reduces fear-potentiated startle in rats as well as marble burying in mice, underscoring its anxiolytic-like properties. At a dose of 10 mg/kg, it enhances dopamine and serotonin release/turnover in the prefrontal cortex[3].When administered orally to fasted rats at doses of 1, 3, or 10 mg/kg, LY404039 shows dose-proportional exposure increases. At a dose of 10 mg/kg, the peak plasma concentration (Cmax) reaches 1528.5 ng/mL with a peak time (Tmax) of 2 hours[1].

LY404039 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01609218 Healthy Volunteer Study Phase 1 Completed - United Kingdom ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Leeds, West Yorkshire, United Kingdom, LS2 9LH 收起 <<
NCT01475136 Hepatic Insufficiency Phase 1 Completed - Germany ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Munich, Germany, 81241 Hungary For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Balatonfüred, Hungary, 8230 收起 <<
NCT01659177 Healthy Participants Phase 1 Withdrawn(The decision to stop... 展开 >> the trial was based on efficacy results in the overall schizophrenia patient population.) 收起 << September 2012 Switzerland ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Mon - Fri from 9 AM to 5 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician. Allschwil, Switzerland, CH-4123 收起 <<

LY404039 参考文献

[1]Linda M Rorick-Kehn, et al. Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-

[2]Seeman P. An agonist at glutamate and dopamine D2 receptors, LY404039. Neuropharmacology. 2013 Mar;66:87-8.

[3]Rorick-Kehn LM, et al. In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonistLY404039 in animal models of psychiatric disorders. Psychopharmacology (Berl). 2007 Jul;193(1):121-36.

LY404039 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.25mL

0.85mL

0.43mL

21.26mL

4.25mL

2.13mL

42.52mL

8.50mL

4.25mL

LY404039 技术信息

CAS号635318-11-5
分子式C7H9NO6S
分子量 235.21
SMILES Code O=C([C@]1(N)CS([C@@]2([H])[C@H](C(O)=O)[C@@]12[H])(=O)=O)O
MDL No. MFCD11974011
别名 pomaglumetad
运输蓝冰
InChI Key AVDUGNCTZRCAHH-MDASVERJSA-N
Pubchem ID 9834591
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案 配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案一

Tags: LY404039 | 635318-11-5 | LY 404039 | LY-404039 | mGluR2/3 Agonist | GPCR/G Protein | Neuronal Signaling | mGluR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | LY404039 纯度/质量文件 | LY404039 生物活性 | LY404039 临床数据 | LY404039 参考文献 | LY404039 实验方案 | LY404039 技术信息

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