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首页-小分子抑制剂&激动剂-GPCR-mGluR-VU6066098
VU6066098

Chemical Structure : VU6066098

CAS No.: 3055537-47-5

VU6066098 (VU-6066098)

货号: PC-27118Not For Human Use, Lab Use Only.

VU6066098 is a potent, selective, and CNS-penetrant mGlu2 negative allosteric modulator (NAM) with IC50 of 77 nM in mGlu2/GIRK assays, with no effect on mGlu3 (IC50>10 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

VU6066098 is a potent, selective, and CNS-penetrant mGlu2 negative allosteric modulator (NAM) with IC50 of 77 nM in mGlu2/GIRK assays, with no effect on mGlu3 (IC50>10 uM).
VU6066098 is inactive (>10 μM) on human mGlu1,3,4,5,7 and a weak PAM of human mGlu8 (EC50 = 5.2 μM, 49% Glu Max).
VU6066098 displays comparable activity (rat mGlu2 IC50 = 111 nM) and selectivity (inactive (>10 μM) on rat mGlu1,3,4,5,7 and a weak PAM of rat mGlu8 (EC50 = 857 nM, 59% Glu Max)).
VU6066098 (1 mg/kg and 10 mg/kg, p.o.,) exerts rapid antidepressant-like effects comparable to ketamine in the rat forced swim test.

物理化学性质&存储条件

分子量 339.35
分子式 C19H15F2N3O
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

6-(2,4-difluorophenyl)-4-(1,3-dimethyl-1H-pyrazol-5-yl)isoindolin-1-one

参考文献

1. Coleman JS, et al. ACS Chem Neurosci. 2026 Jun 23. doi: 10.1021/acschemneuro.6c00324.

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