VU6053371/BI03738809 | mGlu3 PAM | Probechem Biochemicals

Chemical Structure : VU6053371

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VU6053371 (BI03738809)

货号: PC-26985Not For Human Use, Lab Use Only.

VU6053371/BI03738809 is a potent, selective, and centrally active metabotropic glutamate receptor subtype 3 (mGlu3) positive allosteric modulator (PAM) with EC50 of 103 nM and 112 nM for human and rat mGlu3.

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生物&药学活性

VU6053371/BI03738809 is a potent, selective, and centrally active metabotropic glutamate receptor subtype 3 (mGlu3) positive allosteric modulator (PAM) with EC50 of 103 nM and 112 nM for human and rat mGlu3.
VU6053371 is inactive (EC50 > 30 μM) for both human and rat mGlu2, is also selective versus the other mGlu receptors (EC50 > 10 μM)
VU6053371 exhibits EC50 of 90 nM in human mGlu3 CHO cAMP assays, Emax of 41% Glu Max.
VU6053371 dose-dependently enhanced recognition memory in rats with a minimum effective dose (MED) of 3 mg/kg PO and a near maximum response at 10 mg/kg PO in rats.

物理化学性质&存储条件

分子量	386.45
分子式	C19H19FN4O2S
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	4-(3-fluorophenyl)-2-((2-(2-hydroxypropan-2-yl)pyrimidin-5-yl)amino)-5-methylthiophene-3-carboxamide

参考文献

1. Jones CA, et al. ACS Chem Neurosci. 2026 Jun 6. doi: 10.1021/acschemneuro.6c00325.