CVN417 | α6 nAChR inhibitor | Probechem Biochemicals

Chemical Structure : CVN417

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CVN417 (CVN-417, CVN 417)

货号: PC-21112Not For Human Use, Lab Use Only.

CVN417 (CVN-417) is a potent, selective and brain-penetrant α6-containing nicotinic acetylcholine receptor (α6 nAChR) antagonist with Ca2+ flux IC50 of 86 nM.

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生物&药学活性

CVN417 (CVN-417) is a potent, selective and brain-penetrant α6-containing nicotinic acetylcholine receptor (α6 nAChR) antagonist with Ca2+ flux IC50 of 86 nM.
CVN417 showed excellent selectivity over the nAChRα7 isoform (IC50>10 uM), weakly inhibits nAChRα3 and nAChRα4 isoforms (IC50, 2560 and 657 nM, respectively).
CVN417 blocks α6-containing nAChR activity in recombinant cells and reduces firing frequency of noradrenergic neurons in the rodent locus coeruleus.
CVN417 modulates phasic dopaminergic neurotransmission in an impulse-dependent manner.
CVN417 attenuates the behavioral phenotype in rodent model of resting tremor.

物理化学性质&存储条件

分子量	362.86
分子式	C18H23ClN4O2
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	(S)-5-(2-Chloro-4-methoxyphenyl)-1-methyl-N-(1-methylpiperidin-3-yl)-1H-pyrazole-3-carboxamide

参考文献

1. Louisa A Christie, et al. J Med Chem. 2023 Aug 31. doi: 10.1021/acs.jmedchem.3c00630.

CVN417 (CVN-417, CVN 417)

生物&药学活性

物理化学性质&存储条件

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CVN417 (CVN-417, CVN 417)

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物理化学性质&存储条件

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