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MLi-2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MLi-2图片
CAS NO:1627091-47-7
规格:98%
分子量:379.46
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
MLi-2是高效选择的,具有口服活性,可渗透大脑的LRRK2抑制剂。IC50值为0.76nM。
CAS:1627091-47-7
分子式:C21H25N5O2
分子量:379.46
纯度:98%
存储:Store at -20°C

Background:

MLi-2 is an a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.


MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro( IC50=0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50=1.4 nM), and a radioligand competition binding assay (IC50=3.4 nM). MLi-2 has greater than 295-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels[1].


Acute oral and subchronic dosing in MLi-2 mice results in dose-dependent central and peripheral target inhibition over a 24-hour period as measured by dephosphorylation of pSer935 LRRK2. Treatment of MitoPark mice with MLi-2 is well tolerated over a 15-week period at brain and plasma exposures. Morphologic changes in the lung, consistent with enlarged type II pneumocytes, are observed in MLi-2-treated MitoPark mice[1].


[1]. Fell MJ, et al. MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition. J Pharmacol Exp Ther. 2015 Dec;355(3):397-409.