货号	规格	价格	上海	北京	珠海	重庆	武汉
S83735-5mg买3赠1	98.60%	￥690.00 S83735-5mg ￥690.00 现货（买3赠1）	5 5	-	-	-	-
S83735-10mg买3赠1	98.60%	￥900.00 S83735-10mg ￥900.00 现货（买3赠1）	6 6	-	-	-	-
S83735-25mg买3赠1	98.60%	￥1500.00 S83735-25mg ￥1500.00 现货（买3赠1）	5 5	-	-	-	-
S83735-100mg	≥98%	￥2800.00 S83735-100mg ￥2800.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease

靶点：

IC50: 0.76 nM (LRRK2);LRRK2

体外研究：

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.

体内研究：

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.

参考文献：

1. Fell MJ, Mirescu C, Basu K, Cheewatrakoolpong B, DeMong DE, Ellis JM, Hyde LA, Lin Y, Markgraf CG, Mei H, Miller M, Poulet FM, Scott JD, Smith MD, Yin Z, Zhou X, Parker EM, Kennedy ME, Morrow JA. 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.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.635 ml	13.177 ml	26.354 ml
5 mM	0.527 ml	2.635 ml	5.271 ml
10 mM	0.264 ml	1.318 ml	2.635 ml
50 mM	0.053 ml	0.264 ml	0.527 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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