|rel-(2R,6S)-2,6-二甲基-4-(6-(5-(1-甲基环丙氧基)-1H-吲唑-3-基)嘧啶-4-基)吗啉|CsnPharm

CAS No.: 1627091-47-7

MLi-2 is a highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity.

规格	价格	促销价格	库存	数量

400-920-2911

加入购物车大规格询价

产品咨询

400-920-2911

纯度 & 质量文件批次:

生物活性

描述The leucine-rich repeat kinase 2 (LRRK2) is commonly mutated in familial and sporadic Parkinson's disease. Merck LRRK2 inhibitor-2 (MLi-2) is a potent and selective LRRK2 inhibitor with an IC50 value of 0.76nM in a purified LRRK2 kinase assay in vitro. It also exhibited high potency in a cellular assay monitoring the dephosphorylation of pSer935 LRRK2 and a radioligand competition binding assay with IC50 values of 1.4nM and 3.4nM, respectively. In mice, oral administration of MLi-2 dose-dependently reduced phosphorylation of Ser935 with the maximal suppression (>90% reduction) observed at 10mg/kg and higher. The in-diet administration of MLi-2 (3–120mg/kg/day) for 11 days significantly reduced LRRK2 protein level in the kidneys of mice. Treatment with MLi-2 (30mg/kg/day) markedly inhibited pSer935 LRRK2 in the brains of MitoPark mice at 3, 9, and 15 weeks of treatment compared with the vehicle-treated group, but did not stop the progressive motor phenotype or prevented the decline in striatal dopamine, DOPAC, or tyrosine hydroxylase levels in MitoPark mice^[3].
参考文献

实验方案

技术信息

CAS号

1627091-47-7

储存条件

分子式

C21H25N5O2

运输

蓝冰

分子量

379.46

别名

溶解度

DMSO	76.0 mg/mL (200.3 mM)
Ethanol	8.0 mg/mL (21.1 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

请登录您的专属账户