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VU0483605
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VU0483605图片
CAS NO:1623101-11-0
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt446.7
Cas No.1623101-11-0
FormulaC20H10Cl3N3O3
Solubility≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
Chemical Name3-chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide
Canonical SMILESO=C1N(C2=CC=C(NC(C3=C(Cl)C=CC=N3)=O)C=C2Cl)C(C4=CC=CC(Cl)=C41)=O
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

VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1 [1].

The metabotropic glutamate receptors (mGluRs), members of G-protein-coupled receptors, have been involved in a variety of functions in the central and peripheral nervous systems, such as learning, memory, anxiety, and the perception of pain. The mGluRs exist in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, the cerebral cortex, as well as other parts of the brain and in peripheral tissues. Mice deficient in mGluR1 showed severe motor coordination and spatial learning deficient [2].

VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1. VU0483605 displayed EC50 values of 0.39 and 0.36 μM at human and rat mGluR1 receptors, respectively. VU0483605 showed no activity against mGlu4 PAM with the EC50 of >10 μM. VU0483605 potentiated the response to glutamate in cells stably expressing mGlu1 and partially restored the reduction in glutamate-mediated calcium signaling in a mutant cell model of schizophrenia [1].

References:
[1] Cho H P, Garcia-Barrantes P M, Brogan J T, et al.  Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics[J]. ACS chemical biology, 2014, 9(10): 2334-2346.
[2] Conquet F, Bashir Z I, Davies C H, et al.  Motor deficit and impairment of synaptic plasticity in mice lacking mGluR1[J]. Nature, 1994, 372(6503): 237.