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PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC0 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively. PF-06447475 was sufficiently potent in the LRRK2 whole cell assay (WCA; IC50=25 nM) (pS935 end point) to warrant additional profiling. Oral administration of PF-06447475 twice daily for 15 days was well tolerated at doses up to 60 mg kg-1 day-1 (31-fold Cave,0.24h; 70-fold Cmax) with only minimal alterations in RBC parameters, electrolytes, and food consumption without concurrent effects on body weight.
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | G2019S BAC-transgenic mice |
| Formulation | 10% propylene glycol/20% PEG400/70% 9.5% methocellulose |
| Dosages | 100 mg/kg |
| Administration | p.o. |
| Molecular Weight | 305.33 |
| Formula | C17H15N5O |
| CAS Number | 1527473-33-1 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related LRRK2 Products |
|---|
| GNE-7915
GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor with IC50 and Ki of 9 nM and 1 nM, respectively. |
| GNE-9605
GNE-9605 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 19 nM. |
| GSK2578215A
GSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. |
| LRRK2-IN-1
LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. |
| JH-II-127
JH-II-127 is a highly selective LRRK2 inhibitor with an IC50 = 6.5 nM. |
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