JH-II-127

An inhibitor of wild-type and mutant forms of LRRK2

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库存: 现货

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数量
2mg

￥775.00

620.00

- +
5mg

￥1162.00

930.00

- +
10mg

￥1812.00

1450.00

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50mg

￥5400.00

4320.00

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100mg

￥9000.00

7200.00

- +

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Background

JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.IC50 value: 2.2 n(LRRK2-G2019S), 6.6 nM(LRRK2-wild-type), 47.7 nM (LRRK2-A2016T)Target: LRRK2JH-II-127 is a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2. JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 uM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg.

参考文献:
[1]. Hatcher JM, et al. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 Apr 7;6(5):584-589.