LY404039

产品说明书

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Chemical Structure| 635318-11-5 同义名 : pomaglumetad
CAS号 : 635318-11-5
货号 : A358160
分子式 : C7H9NO6S
纯度 : 98%
分子量 : 235.21
MDL号 : MFCD11974011
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
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].
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NCT01659177 Healthy Participants Phase 1 Withdrawn(The decision to stop...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 <<
实验方案
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
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.