product name GNE-7915
Description: GNE-7915 is a novel, highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) inhibitor, with IC50 and Ki of 9 nM and 1 nM, respectively. GEN-7915 has been shown to induce dephosphorylation of LRRK2 in the brain of transgenic mice. GNE-7915 is not reported to cause cellular or genetic toxicity, and has progressed into preclinical studies in cynomolgus monkeys.
References: J Med Chem. 2012 Nov 26;55(22):9416-33
443.40
Formula
C19H21F4N5O3
CAS No.
1374828-69-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 22 mg/mL (49.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: GNE-7915 is also a moderately potent 5-HT2B antagonist according to in vitro functional assays. GNE-7915 demonstrates excellent in vitro DMPK with minimal turnover in human hepatocytes. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In rats, GNE-7915 demonstrates excellent in vivo PK profiles with long half-lives, good oral exposure and high passive permeability. GNE-7915 (50 mg/kg i.p. or p.o.) results in concentration-dependent knockdown of pLRRK2 in the brain of BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation. |
| Animal model | BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation |
| Formulation & Dosage | Dissolved in 1% methylcellulose in water; 50 mg/kg; i.p. injection and p.o. |
| References | J Med Chem. 2012 Nov 26;55(22):9416-33 |
