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.
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. |
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 | 443.40 |
Formula | C19H21F4N5O3 |
CAS Number | 1351761-44-8 |
Purity | >98% |
Solubility | DMSO 10 mM |
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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.