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MLi-2

Chemical Structure : MLi-2

CAS No.: 1627091-47-7

MLi-2 (LRRK2 inhibitor MLi-2)

货号: PC-21889Not For Human Use, Lab Use Only.

MLi-2 is a potent, highly selective, orally available, brain-penetrant inhibitor of LRRK2 with IC50 of 0.76 nM, pSer935 LRRK2 IC50 of 1.4 nM.

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5 mg ¥1180 In stock
10 mg ¥1780 In stock
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50 mg ¥4580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MLi-2 is a potent, highly selective, orally available, brain-penetrant inhibitor of LRRK2 with IC50 of 0.76 nM, pSer935 LRRK2 IC50 of 1.4 nM.
MLi-2 shows an IC50 of 3.4 nM in a radioligand competition binding assay, > 95-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels.
MLi-2 signficantly reduces the ratio of phosphorylated Ser935 LRRK2 (pS935) to total LRRK2 in the mouse cortex in both single dose and 11-day in-diet studies.
MLi-2 significantly reduces pS935 in a dose dependent manner (1–100 mg/kg) 1 h post treatment in rats.

物理化学性质&存储条件

分子量 379.46
分子式 C21H25N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

rel-(2S,6R)-2,6-Dimethyl-4-(6-(5-(1-methylcyclopropoxy)-1H-indazol-3-yl)pyrimidin-4-yl)morpholine

参考文献

1. Scott JD, et al. J Med Chem. 2017 Apr 13;60(7):2983-2992.

2. Fell MJ, et al. J Pharmacol Exp Ther. 2015 Dec;355(3):397-409.

3. Volpicelli-Daley LA, et al. J Neurosci. 2016 Jul 13;36(28):7415-27.

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