Xcess/ADX47273-Xcessbio Biosciences Inc/2mg/M60433-2s,Xcess,,Xcess,xcessbio,Xcess Biosciences Inc,+,,Array.Array蚂蚁淘厂家直采.

产品名称：Xcess/ADX47273-Xcessbio Biosciences Inc/2mg/M60433-2s

产品编号：M60433-2s

市场价：¥1780.00

场地：美国(厂家直采)

产品分类：蛋白类>聚合物>

联系QQ：1570468124

电话号码：4000-520-616

邮箱： info@ebiomall.com

美元价：$89.00

品牌： Xcess

公司：Xcess Biosciences, Inc

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Details

Product Information

Molecular Weight:	369.36
Formula:	C₂₀H₁₇F₂N₃O₂
Purity:	>98%
CAS#:	851881-60-2
Solubility:	DMSO: ≥ 31 mg/mL
Chemical Name:	(S)-(4-fluorophenyl)(3-(3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)methanone
Storage:	Powder -20^oC 3 years 4^oC 2 yearsIn solvent -80^oC 6 months-20^oC 1 month

Biological Activity:

ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM). IC50 value: 170 nM(EC50) [1] [2] Target: positive allosteric modulator (PAM) of mGluR5

How to use:

in vitro: ADX-47273 increased (9-fold) the response to threshold concentration of glutamate (50 nM) in fluorometric Ca(2+) assays (EC(50) = 170 nM) in human embryonic kidney 293 cells expressing rat mGlu5. ADX47273 dose-dependently shifted mGlu5 receptor glutamate response curve to the left (9-fold at 1 microM) and competed for binding of [(3)H]2-methyl-6-(phenylethynyl)pyridine (K(i) = 4.3 microM), but not [(3)H]quisqualate [2].

in vivo: ADX47273 increased extracellular signal-regulated kinase and cAMP-responsive element-binding protein phosphorylation in hippocampus and prefrontal cortex, both of which are critical for glutamate-mediated signal transduction mechanisms. In models sensitive to antipsychotic drug treatment, ADX47273 reduced rat-conditioned avoidance responding [minimal effective dose (MED) = 30 mg/kg i.p.] and decreased mouse apomorphine-induced climbing (MED = 100 mg/kg i.p.), with little effect on stereotypy or catalepsy [2]. ADX47273 had no effect on single-session and multi-session extinction, but administration of ADX47273 after a single retrieval trial enhanced subsequent fear extinction learning [3].

Reference:

[1]. de Paulis T, et al. Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. J Med Chem. 2006 Jun 1;49(11):3332-44.

[2]. Liu F, et al. ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive

[3]. Xu J, et al. Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning. Learn Mem. 2013 Jul 18;20(8):438-45.

品牌介绍

Xcess Biosciences，Inc.（XcessBio）由一群来自学术界和制药/生物技术行业的顶尖科学家于2008年成立，他们在药物化学，生物化学，分子和细胞生物学领域拥有丰富的专业知识。结合我们的合作者和顾问网络，我们致力于开发高质量的产品并提供最佳的服务，以满足生物医学研究中未满足的需求。

XcessBio的总部位于加利福尼亚州圣地亚哥，在最先进的研发设施中运营，设有化学合成实验室，分子和细胞生物学实验室以及分析质量控制实验室。

XcessBio一直为美国许多顶级制药，生物技术和试剂公司提供CRO服务和OEM产品，现在，我们将最好的产品和服务直接扩展到整个生命科学界。

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