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.
 |
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 | |
|---|---|
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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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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