FX 2149
FX 2149 is a blood-brain barrier-permeable LRRK2 inhibitor. FX 2149 inhibits the GTP-binding activity of LRRK2, reduces the kinase activity of LRRK2, and attenuates LPS (HY-D1056)-induced upregulation of LRRK2. FX 2149 alleviates mutant LRRK2-induced neurodegeneration, microglial activation, static aggregation of mitochondria and lysosomes, reduces apoptosis, and improves mitochondrial and lysosomal motility deficits in neurites. FX 2149 can be used in research related to Parkinson's disease.
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- No. CAS: 1842427-90-0
- Fòrmula: C15H17N3O3S
- Peso molecular:319.38
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
FX 2149 (50-200 nM; 48 h) attenuates LRRK2G2019S-induced toxicity in SH-SY5Y cells, increasing cell viability and reducing apoptosis at concentrations ≥50 nM, with 100 nM showing efficacy equivalent to 10 nM compound 68[1].
FX 2149 (100 nM; 48 h) attenuates LRRK2R1441C-induced mitochondrial transport impairments in SH-SY5Y cells by reducing stationary mitochondria and increasing motile mitochondrial percentage and run length[2].
FX 2149 (100 nM; 48 h) attenuates LRRK2R1441C-induced lysosomal transport impairments in SH-SY5Y cells by reducing stationary lysosomes and increasing motile lysosomal percentage and run length[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human neuroblastoma SH-SY5Y cells expressing G2019S-LRRK2
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Concentration:50 nM, 100 nM, 200 nM
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Incubation Time:48 h
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Result:Increased the viability of G2019S-LRRK2-expressing cells compared to vehicle-treated cells.
Reduced the percentage of TUNEL-positive G2019S-LRRK2-expressing cells to levels.
FX2149 (10 mg/kg; i.p.; twice daily for 3 consecutive days) reduces LPS-induced microglial activation by 57% in the substantia nigra of LRRK2G2019S-BAC transgenic mice, and inhibits the upregulation and phosphorylation of LRRK2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:G2019S-LRRK2-BAC transgenic (6-12 weeks of age)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Reduced brain LRRK2 GTP binding activity to levels.
Significantly reduced brain LRRK2 kinase activity.
Reduced 4E-BP phosphorylation to 15% of the untreated transgenic control group.
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Animal Model:G2019S-LRRK2-BAC transgenic (6-12 weeks of age)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single pre-LPS dose followed by twice daily doses; 3 days
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Result:Significantly reduced LPS-induced LRRK2 expression and phosphorylated-LRRK2 immunoactivity in the substantia nigra.
Reduced LPS-induced isolectin B4 positive immunostaining to ~43% of the LPS-alone treated group, representing a 57% reduction in microglia activation.
Left dopaminergic neuron marker (TH) immunostaining unchanged across groups.
Chemical Information
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No. CAS 1842427-90-0
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Peso molecular 319.38
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Fòrmula C15H17N3O3S
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SMILES
O=C(NCCC)C=1C=CC=C(C1)NS(=O)(=O)C=2C=NC=CC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Li T, et al. A novel GTP-binding inhibitor, FX2149, attenuates LRRK2 toxicity in Parkinson's disease models. PloS one. 2015;10(3):e0122461. [Content Brief]
[2]. Thomas JM, et al. 68 and FX2149 Attenuate Mutant LRRK2-R1441C-Induced Neural Transport Impairment. Frontiers in aging neuroscience. 2016;8:337. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FX 2149 Related Classifications
HY-169900 Related Classifications
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