Chemical Structure : GSK2820986A
CAS No.:
GSK2820986A
(GSK-2820986A)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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490.00
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Formula
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C28H28ClN3O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Collingridge J, et al. J Biol Chem. 2026 Oct 13:113644.
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