化学性质
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 235.21 |
Cas No. | 635318-11-5 |
Formula | C7H9NO6S |
Solubility | insoluble in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | (1R,4S,5S,6S)-4-amino-2,2-dioxo-2λ6-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid |
Canonical SMILES | C1C(C2C(C2S1(=O)=O)C(=O)O)(C(=O)O)N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
资料参考
LY404039是一种有效的和高选择性的重组人类mGlu2和mGlu3受体以及大鼠神经元表达自身mGlu2/3受体的激动剂,Ki值分别为149\92和88 nM[1].
对毛喉素刺激的cAMP生成的抑制能力表明LY404039是一种纳摩尔级别有效的人类mGlu2(EC50 = 23 nM)和mGlu3(EC50 = 48 nM)受体的激动剂.此外,LY404039可在大鼠纹状体多刺神经元中浓度依赖地降低兴奋性突触后电位(RPSP)(EC50 = 141 nM).LY404039也可在大鼠前额叶皮层切片中抑制5-HT诱导的突触后电位频率(EC50 = 82.3 nM)[1].
参考文献:
[1] Rorick-Kehn LM1, Johnson BG, Burkey JL, Wright RA, Calligaro DO, Marek GJ, Nisenbaum ES, Catlow JT, Kingston AE, Giera DD, Herin MF, Monn JA,McKinzie DL, Schoepp DD. 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]-hexane-4,6-dicarboxylic acid (LY404039). J Pharmacol Exp Ther. 2007 Apr;321(1):308-17. Epub 2007 Jan 4. J Pharmacol Exp Ther. 2007 Apr;321(1):308-17. Epub 2007 Jan 4.