MLi-2|1627091-47-7|-陌孚医药/Medlife

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MLi-2

目录号: PL06801 纯度: ≥99%

CAS No. :1627091-47-7

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中文名称	MLi-2
中文别名	MLi-2
英文名称	MLi-2
英文别名	MLi-2;MLi2;MLi-2 - Bio-X;(2~{r},6~{s})-2,6-Dimethyl-4-[6-[5-(1-Methylcyclopropyl)oxy-1~{h}-Indazol-3-Yl]pyrimidin-4-Yl]morpholine;(2S,6R)-2,6-dimethyl-4-(6-(5-(1-methylcyclopropoxy)-1H-indazol-3-yl)pyrimidin-4-yl)morpholine;S9694;J3.645.913A;Q27225595;cis-2,6-dimethyl-4-(6-(5-(1-methylcyclopropoxy)-1H-indazol-3-yl)pyrimidin-4-yl)morpholine;(2R,6S)-2,6-dimethyl-4-[6-[5-(1-methylcyclopropyl)oxy-1H-indazol-3;Merck lrrk2 inhibitor-2;GTPL11663;AT22709;compound 1 [PMID: 28245354];cis-2,6-dimethyl-4-(6-(5-(1-methylcyclopropoxy)-1H-indazol-3-yl)pyrimidin-4-y;MLi-2-Bio-X
Cas No.	1627091-47-7
分子式	C₂₁H₂₅N₅O₂
分子量	379.46
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	MLi-2 是一种具有口服活性的，高选择性 LRRK2 抑制剂，IC₅₀ 为 0.76 nM。MLi-2 具有用于帕金森氏病的潜力。
生物活性	MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC 50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.
性状	Solid
IC50 & Target[1][2]	IC50: 0.76 nM (LRRK2)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

溶解度数据	In Vitro: DMSO : 50 mg/mL (131.77 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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