VU0650786
目录号: PL07147 纯度: ≥99%
CAS No. :1809085-30-0
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中文名称
VU0650786
中文别名
化合物VU0650786
英文名称
VU0650786
英文别名
VU0650786;GTPL10237;BDBM50122111;VU 0650786;(7R)-2-[(5-Chloropyridin-2-yl)oxymethyl]-5-(2-fluoropyridin-3-yl)-7-methyl-6,7-dihydropyrazolo[1,5-a]pyrazin-4-one;(7R)-2-{[(5-chloropyridin-2-yl)oxy]methyl}-5-(2-fluoropyridin-3-yl)-7-methyl-4H,5H,6H,7H-pyrazolo[1,5-a]pyrazin-4-one;CID 122190433;Pyrazolo[1,5-a]pyrazin-4(5H)-one, 2-[[(5-chloro-2-pyridinyl)oxy]methyl]-5-(2-fluoro-3-pyridinyl)-6,7-dihydro-7-methyl-, (7R)-;inhibit,anxiolytic activity,antidepressant,Inhibitor,VU-0650786,mGlu3 NAM,VU0650786,mGluR,Metabotropic glutamate receptors,VU 0650786
Cas No.
1809085-30-0
分子式
C18H15ClFN5O2
分子量
387.80
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
VU0650786 是一种有效的,能透过中枢神经系统的,选择性谷氨酸受体亚型 3 的负变构调节剂 (mGlu3 NAM),IC50 值为 392 nM。VU0650786 在啮齿动物中具有抗抑郁和抗焦虑活性。
生物活性
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC 50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
性状
Solid
IC50 & Target[1][2]
mGluR3 392 nM (IC50)
体内研究(In Vivo)
VU0650786 (VU786) (i.p., 30 mg/kg) increases the proportion of c-Fos-positive cells by approximately 4-fold, enhances synaptic strength in cone cell subpopulations, weakens thalamocortical long-term depression (LTD), and reduces passive coping in acute models of antidepressant-like activity in inducible cFos-EGFP mice.
The pharmacokinetic parameters of VU0650786 (compound 106) in rats.
Parameters IV (0.2 mg/kg)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Engers JL, et al. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J Med Chem. 2015 Sep 24;58(18):7485-500.
[2]. Max E Joffe, et al. mGlu2 and mGlu3 Negative Allosteric Modulators Divergently Enhance Thalamocortical Transmission and Exert Rapid Antidepressant-like Effects. Neuron. 2020 Jan 8;105(1):46-59.e3.
溶解度数据
In Vitro: DMSO : 250 mg/mL (644.66 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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