TRPC3 antagonist 60a

Chemical Structure : TRPC3 antagonist 60a

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货号: PC-23549Not For Human Use, Lab Use Only.

TRPC3 antagonist 60a is a potent, selective TRPC3 antagonist with IC50 of 60 nM, has significant neuronal protective abilities.

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生物&药学活性

TRPC3 antagonist 60a is a potent, selective TRPC3 antagonist with IC50 of 60 nM, has significant neuronal protective abilities.
TRPC3 antagonist 60a has 4-fold increased potency compared with that of JW-65.
TRPC3 antagonist 60a has no detectable inhibition on TRPC3-related ion channels (TRPC6, TRPC7, TRPA1, TRPV1, and TRPM8), especially its structurally close homologs TRPC6/7.
TRPC3 antagonist 60a corrects neuronal dysfunction induced by β-amyloid in vitro β-amyloidosis model.
TRPC3 antagonist 60a also mitigates 7PA2-induced overactivation of microglia and astrocytes, and corrects the loss of neuroprotective proteins (e.g., Syn I and PSD95) in the 7PA2-treated cells.

物理化学性质&存储条件

分子量	431.24
分子式	C18H15Cl2F3N4O
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	3,4-dichloro-1-(4-(4-((ethylamino)methyl)-5-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)pyridin-2(1H)-one

参考文献

1. Wang J, et al. Bioorg Med Chem. 2024 Nov 26;117:118021.