[CAS NO. 1374828-69-9] GNE-0877
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PRODUCTS SPECIFICATIONS [1374828-69-9]
Catalog
SLK-S7367
Brand
Selleck
CAS
1374828-69-9
DESCRIPTION [1374828-69-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 339.32 |
| Molecular Formula | C14H16F3N7 |
| SMILES | N#CC(C)(C)N1N=C(C)C(NC2=NC=C(C(F)(F)F)C(NC)=N2)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9471 mL | 14.7354 mL | 29.4707 mL |
| 5 mM | 0.5894 mL | 2.9471 mL | 5.8941 mL |
| 10 mM | 0.2947 mL | 1.4735 mL | 2.9471 mL |
| 50 mM | 0.0589 mL | 0.2947 mL | 0.5894 mL |
Description
GNE-0877 (DNL201) is a highly potent and selective inhibitor with of 0.7 nM.
Targets
| LRRK2 [1] |
| 0.7 nM(Ki) |
In vitro
GNE-0877 significantly inhibits LRRK2 cellular activity with IC50 of 3 nM, and shows low turnover in human liver microsomes and hepatocytes. Besides, GNE-0877 is also a reversible CYP1A2 inhibitor with IC50 of 0.7 μM.
In vivo
In vivo, GNE-0877 shows good oral bioavailability and brain penetration. GNE-0877 inhibits in vivo LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.
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