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首页-小分子抑制剂&激动剂-GPCR-mGluR-VU 0650786
VU 0650786

Chemical Structure : VU 0650786

CAS No.: 1809085-30-0

VU 0650786 (VU0650786;VU-0650786)

货号: PC-60936Not For Human Use, Lab Use Only.

VU 0650786 (VU0650786, VU-0650786) is a potent and selective, CNS penetrant mGlu3 negative allosteric modulator with IC50 of 392 nM, with no significant activity against other mGlus (IC50>10 uM).

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生物&药学活性

VU 0650786 (VU0650786, VU-0650786) is a potent and selective, CNS penetrant mGlu3 negative allosteric modulator with IC50 of 392 nM, with no significant activity against other mGlus (IC50>10 uM).
VU 0650786 displays suitability for use in rodent behavioral models, and demonstrates efficacy in models in vivo.
VU 0650786 reverses disrupted contextual fear memory caused by mGlu2/3 agonist LY379268 in vivo.

物理化学性质&存储条件

分子量 387.799
分子式 C18H15ClFN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-2-(((5-Chloropyridin-2-yl)oxy)methyl)-5-(2-fluoropyridin-3-yl)-7-methyl-6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one

参考文献

1. Engers JL, et al. J Med Chem. 2015 Sep 24;58(18):7485-500.

2. Walker AG, et al. Neuropsychopharmacology. 2017 Dec;42(13):2553-2566.

3. Engers JL, et al. ACS Med Chem Lett. 2017 Aug 15;8(9):925-930.

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