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GNE-7915 is a moderately potent 5-HT2B antagonist. GNE-7915 demonstrates excellent in vitro DMPK with minimal turnover in human hepatocytes. GNE-7915 demonstrates excellent in vivo PK profiles with long half-lives, good oral exposure and high passive permeability.
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Source | CNS Neurosci Ther (2017). Figure 2. GNE-7915 |
| Method | Western blot | |
| Cell Lines | WT mice | |
| Concentrations | 1 and 3 μM | |
| Incubation Time | 2-h | |
| Results | In contrast, GSK2578215A and GNE-7915 at all concentrations had no effect on DA release and recovery. Western blot confirmed the dose–response inhibition by the LRRK2 inhibitions |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation |
| Formulation | Suspended in 1% microcrystalline cellulose |
| Dosages | 50 mg/kg |
| Administration | i.p. ; p.o. |
| Molecular Weight | 443.40 |
| Formula | C19H21F4N5O3 |
| CAS Number | 1351761-44-8 |
| Solubility (25°C) | DMSO ≥ 60 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-9605
GNE-9605 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 19 nM. |
| PF-06447475
PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC0 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively. |
| 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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