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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 | |
|---|---|
| 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 |
|---|
| LRRK2-IN-8
LRRK2-IN-8 is a LRRK2 inhibitor. |
| LRRK2/NUAK1/TYK2-IN-1
LRRK2/NUAK1/TYK2-IN-1 (conpound 226) shows inhibitory activity toward LRRK2 (Wt), LRRK2 (G2019), TYK2 and NUAK1, with IC50 values lower than 10 nM. |
| EB-42486
EB-42486 is a novel potent and highly selective inhibitor of G2019S-LRRK2 (IC50 < 0.2 nM). |
| CZC-54252
CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for human wild type LRRK2 and G2019S LRRK2, respectively. |
| WAY-333491
WAY-333491 is a LRRK2 kinase inhibitor. |
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