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VU 0424465
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。
VU 0424465图片
规格:98%
分子量:326.37
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
VU 0424465 是一种有效的部分 PAM(正变构调节剂)激动剂,用于 mGlu5 介导的 iCa2+ 动员。
货号:ajcx27870
CAS:1428630-85-6
分子式:C19H19FN2O2
分子量:326.37
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Potent mGlu5 positive allosteric modulator (EC50 = 1.5 nM) and agonist (EC50 = 171 nM; maximum effect is 65% that of glutamate). Binds allosteric site with high affinity (Ki = 11.8 nM). Increases maximum response to glutamate by 30%. Exhibits bias towards signaling via IP1 and ERK1/2 over iCa2+ in HEK293 and neuronal cells, and activates Gs in HEK 293 cells. Induces epileptiform activity in CA3 hippocampal neurons in vitro and convulsions in vivo.


Rook et al (2013) Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol.Psychiatry. 73 501 PMID:23140665 |Sengmany et al (2017) Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology 115 60 PMID:27392634 |Nasrallah et al (2018) Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs. Sci.Rep. 8 4407 PMID:29535347