HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant (IC50 for LRRK2-wild-type ~20.3 nM and LRRK2-[G2019S] ~3.2 nM). It significantly inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1−0.3 μM in cells. HG-10-102-01 is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg. It may represent a good lead compound for a subset of Parkinson's disease.
CAS Number: 1351758-81-0
Molecular Weight: 377.83
Chemical Name: (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
HG-10-102-01was used at 0.3-1.0 µM final concentration in vitro and in cellular assays.
HG-10-102-01 was intraperitoneally (IP) dosed to mice at 50 mg/kg once per day.
- Choi HG, et al. Brain Penetrant LRRK2 Inhibitorn (2012) ACS Med. Chem. Lett., 2012, 3 (8), 658–662.
- Chen H, et al. Discovery of Selective LRRK2 Inhibitors Guided by Computational Analysis and Molecular Modeling. (2012) Journal of Medicinal Chemistry. 55(11), 5536-5545.
Products are for research use only. Not for human use.
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