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FX2149

Chemical Structure : FX2149

CAS No.: 1842427-90-0

FX2149 (FX 2149)

Catalog No.: PC-49821Not For Human Use, Lab Use Only.

FX2149 (FX 2149) is a potent, BBB permeable inhibitor of LRRK2 GTP binding activity with IC90 of 10 nM, reduces PD-linked mutant LRRK2 variants (G2019S and R1441C) that bound with GTP.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

FX2149 (FX 2149) is a potent, BBB permeable inhibitor of LRRK2 GTP binding activity with IC90 of 10 nM, reduces PD-linked mutant LRRK2 variants (G2019S and R1441C) that bound with GTP.
FX2149 potently inhibits LRRK2 GTP binding and kinase activity in vitro.
FX2149 at 100 nM concentration significantly reduced G2019S-LRRK2 phosphorylation at residues S935 and S2032 by 90% in cell-free assays.
FX2149 (100 nM) attenuated G2019S-LRRK2-induced neuronal degeneration in SH-SY5Y cells.
FX2149 (10 mg/kg) is more efficient in reducing LRRK2 GTP binding and kinase activities in transgenic mice brains than LRRK2 inhibitor 68.
FX2149 (10 mg/kg) reduced LPS-induced microglia activation and LRRK2 upregulation in mice.
FX2149 attenuates LRRK2-R1441C-induced mitochondrial and lysosomal transport impairments.

Physicochemical Properties

M.Wt 319.38
Formula C15H17N3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-Propyl-3-(pyridine-3-sulfonamido)benzamide

References

1. Li T, et al. PLoS One. 2015 Mar 27;10(3):e0122461.

2. Thomas JM, et al. Front Aging Neurosci. 2017 Jan 10;8:337.

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