VU0477573 | mGlu5 NAM | Probechem Biochemicals

Chemical Structure : VU0477573

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VU0477573 (VU-0477573, VU 0477573)

货号: PC-60820Not For Human Use, Lab Use Only.

VU0477573 is a potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca2+ assay IC50 of 32 nM.

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生物&药学活性

VU0477573 is a potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca2+ assay IC50 of 32 nM.
VU0477573 shows no activity against the other mGlu receptor subtypes (>10 uM).
VU0477573 exhibits full occupancy of the MPEP site, does not completely inhibit maximal effects of mGlu5 agonists on intracellular calcium mobilization, inositol phosphate (IP) accumulation, or inhibition of synaptic transmission at the hippocampal Schaffer collateral-CA1 synapse.
VU0477573 acts as a full NAM when measuring effects on mGlu5-mediated ERK1/2 phosphorylation.
VU0477573 shows robust efficacy, comparable to the mGlu5 NAM MTEP, in models of anxiolytic activity.

物理化学性质&存储条件

分子量	296.345
分子式	C18H17FN2O
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	N,N-diethyl-5-((3-fluorophenyl)ethynyl)picolinamide

参考文献

1. Nickols HH, et al. J Pharmacol Exp Ther. 2016 Jan;356(1):123-36.

VU0477573 (VU-0477573, VU 0477573)

生物&药学活性

物理化学性质&存储条件

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VU0477573 (VU-0477573, VU 0477573)

生物&药学活性

物理化学性质&存储条件

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