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首页-小分子抑制剂&激动剂-GPCR-mGluR-VU6081679
VU6081679

Chemical Structure : VU6081679

CAS No.:

VU6081679 (VU 6081679)

货号: PC-27729Not For Human Use, Lab Use Only.

VU6081679 is a potent, CNS penetrant, orally bioavailable metabotropic glutamate receptor subtype 8 (mGlu8) positive allosteric modulator (PAM) with EC50 of 211/190/162 nM for rat/mouse/human Glu8 receptors respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

VU6081679 is a potent, CNS penetrant, orally bioavailable metabotropic glutamate receptor subtype 8 (mGlu8) positive allosteric modulator (PAM) with EC50 of 211/190/162 nM for rat/mouse/human Glu8 receptors respectively.
VU6081679 is selective over CNS expressed Group III mGlus, mGlu4 and mGlu7, as well as the Group II mGlus, mGlu2 and mGlu3.
VU6081679 displays weak PAM activity at the two Group I mGlu receptors (mGlu1 EC50 = 295 nM (42% Glu Max); mGlu5 EC50 = 1290 nM (49% Glu Max)).
VU6081679 displays a good rodent PK profile, allowing for in vivo evaluation.
VU6081679 exhibits efficacy in an acute haloperidol-induced catalepsy model of Parkinson's disease in two rodent species.

物理化学性质&存储条件

分子量 421.43
分子式 C22H20FN5O3
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-(3,4-Dimethoxyphenyl)-2-((5-fluoro-6-(1-methyl-1H-pyrazol-4-yl)­pyridin-3-yl)­methyl)­pyridazin-3­(2H)-one

参考文献

1. Alexa E Richardson, et al. ACS Chem Neurosci. 2026 Aug 5;17(15):3023-3034.

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