HG-10-102-01,LRRK2Inhibitor
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產品名稱: HG-10-102-01,LRRK2Inhibitor
產品型號: M60061-2s
產品展商: 其它品牌
產品文檔: 無相關文檔
簡單介紹
HG-10-102-01,LRRK2Inhibitor
HG-10-102-01,LRRK2Inhibitor
的詳細介紹
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.?
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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.
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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.
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Products are for research use only. Not for human use.
