货号	规格	价格	上海	北京	珠海	重庆	武汉
S89806-5mg促销	99.60%	￥1120.00 ￥896.00 S89806-5mg ￥896.00 现货	6 6	-	-	-	-
S89806-10mg促销	99.60%	￥1800.00 ￥1440.00 S89806-10mg ￥1440.00 现货	6 6	-	-	-	-
S89806-25mg促销	99.60%	￥3600.00 ￥2880.00 S89806-25mg ￥2880.00 现货	6 6	-	-	-	-

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产品描述：

VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM).

靶点：

GluR

体内研究：

VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice

参考文献：

1. Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology. 2017 Mar 15;115:60-72. doi: 10.1016/j.neuropharm.2016.07.001. Epub 2016 Jul 5. PubMed PMID: 27392634; PubMed Central PMCID: PMC5217481. 2. Kiritoshi T, Ji G, Neugebauer V. Rescue of Impaired mGluR5-Driven Endocannabinoid Signaling Restores Prefrontal Cortical Output to Inhibit Pain in Arthritic Rats. J Neurosci. 2016 Jan 20;36(3):837-50. doi: 10.1523/JNEUROSCI.4047-15.2016. PubMed PMID: 26791214; PubMed Central PMCID: PMC4719019. 3. Notartomaso S, Mascio G, Scarselli P, Martinello K, Fucile S, Gradini R, Bruno V, Battaglia G, Nicoletti F. Expression of the K(+)/Cl(-) cotransporter, KCC2, in cerebellar Purkinje cells is regulated by group-I metabotropic glutamate receptors. Neuropharmacology. 2017 Mar 15;115:51-59. doi: 10.1016/j.neuropharm.2016.07.032. Epub 2016 Aug 3. PubMed PMID: 27498071. 4. D'Amore V, Raaijmakers RH, Santolini I, van Rijn CM, Ngomba RT, Nicoletti F, van Luijtelaar G. The anti-absence effect of mGlu5 receptor amplification with VU0360172 is maintained during and after antiepileptogenesis. Pharmacol Biochem Behav. 2016 Jul-Aug;146-147:50-9. doi: 10.1016/j.pbb.2016.05.004. Epub 2016 May 10. PubMed PMID: 27178815.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.398 ml	16.988 ml	33.977 ml
5 mM	0.68 ml	3.398 ml	6.795 ml
10 mM	0.34 ml	1.699 ml	3.398 ml
50 mM	0.068 ml	0.34 ml	0.68 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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