VU 0357121, mGlu 5 受体的异构调节剂

mGluR5 Selective Agonists | Antagonists
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Compound libraries (12332)

基本描述

英文别名 4-butoxy-N-(2,4-difluorophenyl)benzamide
规格或纯度 Moligand™, 10mM in DMSO
英文名称 VU 0357121
生化机理 VU0357121 是一种新型 mGlu5 阳性异位调节剂 (PAM),EC50 为 33 nM,对其他 mGlu 受体亚型无活性或极弱的拮抗作用。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 变构调节剂
作用机制 mGlu 5 受体的异构调节剂
产品介绍

VU0357121是新型的mGlu5R正向变构调节剂,EC50为33 nM。A novel allosteric modulator of mGluR-5 receptors

Information

VU0357121 is a novel positive allosteric modulator (PAM) ofmGlu5withEC50of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.
In vitro

VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration−response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line.

In vivo


Cell Data

cell lines:Human thyroid anaplastic carcinoma cell line, CAL-62 cell

Concentrations:

Incubation Time:

Powder Purity:≥99%

关联靶点(人)

GRM5 Tchem 代谢型谷氨酸受体 5(Metabotropic glutamate receptor 5) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CCCCOC1=CC=C(C=C1)C(=O)NC2=C(F)C=C(F)C=C2
分子量 305.32

化学和物理性质

溶解性 Solubility (25°C) In vitro      

安全和危险性(GHS)

技术规格说明书

Concentration 9-11(mmol/L)
Proton NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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