产品详情
简单介绍：
HG-10-102-01,LRRK2Inhibitor
详情介绍：
Product Information
| Molecular Weight: | 377.83 |
| Formula: | C17H20ClN5O3 |
| Purity: | ≥98% |
| CAS#: | 1351758-81-0 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
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.
How to Use:
- In vitro: HG-10-102-01was used at 0.3-1.0 µM final concentration in vitro and in cellular assays.
- In vivo: HG-10-102-01 was intraperitoneally (IP) dosed to mice at 50 mg/kg once per day.
Reference:
- 1. Choi HG, et al. Brain Penetrant LRRK2 Inhibitorn (2012) ACS Med. Chem. Lett., 2012, 3 (8), 658–662.
- 2. 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.
相关文章
