GSK2820986A | TRPC3 inhibitor | Probechem Biochemicals

Chemical Structure : GSK2820986A

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GSK2820986A (GSK-2820986A)

货号: PC-28514Not For Human Use, Lab Use Only.

GSK2820986A (GSK-986) is a highly potent, selective TRPC3 inhibitor with pIC50 values of 8.15 (IC50=7 nM, hTRPC3) and 8.7 (IC50=2 nM, rTRPC3), respectively in FLIPR assays.

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生物&药学活性

GSK2820986A (GSK-986) is a highly potent, selective TRPC3 inhibitor with pIC50 values of 8.15 (IC50=7 nM, hTRPC3) and 8.7 (IC50=2 nM, rTRPC3), respectively in FLIPR assays.
GSK-986 is about 10-fold selectively for TRPC3 over the related TRPC6 channel in the FLIPR assay.
GSK-986 inhibits TRPC3 in the nanomolar range with pIC50 values of 7.43 (IC50=37 nM, hTRPC3) and 7.2 (IC50=63 nM, mTRPC3), respectively in human and mouse TRPC3-overexpressing HEK293 cells by patch clamp planar array electrophysiology assays.
TRPC3 mutation Q555A impairs inhibition by GSK-986.
GSK2820986A (GSK-986) is a useful tool for TRPC3 inhibition with selectivity over TRPC6.

物理化学性质&存储条件

分子量	490.00
分子式	C28H28ClN3O3
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-(2-chloro-4-(2-hydroxyethoxy)phenyl)-1-methyl-1H-pyrazol-4-yl)((2S,5S)-2-methyl-5-(naphthalen-1-yl)pyrrolidin-1-yl)methanone

参考文献

1. Collingridge J, et al. J Biol Chem. 2026 Oct 13:113644.

GSK2820986A (GSK-2820986A)

生物&药学活性

物理化学性质&存储条件

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GSK2820986A (GSK-2820986A)

生物&药学活性

物理化学性质&存储条件

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