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GNE-9605 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. Leucine-rich repeat kinase 2 (LRRK2) has drawn significant interest in the neuroscience research community because it is one of the most compelling targets for a potential disease-modifying Parkinson's disease therapy.
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | G2019S LRRK2 transgenic mice |
| Formulation | 60% NMP |
| Dosages | 10, 50 mg/kg |
| Administration | i.p. |
| 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.
| Molecular Weight | 449.83 |
| Formula | C17H20ClF4N7O |
| CAS Number | 1536200-31-3 |
| Purity | >98% |
| Solubility | DMSO 60 mg/mL |
| Storage | at -20°C |
| Related LRRK2 Products |
|---|
| MLi-2
MLi-2 is a highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM). |
| PFE-360
PFE-360, also known as PF-06685360, is a potent and selective, brain penetrated inhibitor of LRRK2 kinase. |
| CZC 25146
CZC 25146 is a potent LRRK2 inhibitor. |
| JH-II-127
JH-II-127 is a highly selective LRRK2 inhibitor with an IC50 = 6.5 nM. |
| LRRK2-IN-1
LRRK2-IN-1 is useful in treatment of Parkinson's disease. |
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