MW-150|1628502-91-9|-陌孚医药/Medlife

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MW-150

目录号: PL08716 纯度: ≥99%

CAS No. :1628502-91-9

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中文名称	MW-150
中文别名	6-(4-甲基哌嗪-1-基)-3-(萘-2-基)-4-(吡啶-4-基)哒嗪
英文名称	MW-150
英文别名	6-(4-Methylpiperazin-1-Yl)-3-(Naphthalen-2-Yl)-4-(Pyridin-4-Yl)pyridazine;EPZ68T461K;GTPL10524;CIIVUDIZZJLXCN-UHFFFAOYSA-N;MW150;compound 8 [PMID: 25676389];compound 11 [PMID: 30978288];compound 27 [WO2014145485A2];Q27453797;6-(4-methylpiperazin-1-yl)-3-naphthalen-2-yl-4-pyridin-4-ylpyridazine;6-(4-Methyl-piperazin-1-yl)-(2-naphthalen-2-yl)-4-pyridin-4-ylpyridazine;Pyridazine, 6-(4-methyl-1-pipe;MW01-18-150SRM;MW-150
Cas No.	1628502-91-9
分子式	C₂₄H₂₃N₅
分子量	381.47
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

MW-150 (MW01-18-150SRM) 是一种选择性，口服有效的，可透过神经系统的 p38α MAPK 抑制剂，K_i 值为 101 nM。MW-150 抑制内源性 p38α MAPK 在活化的神经胶质中磷酸化内源性底物 MK2 的能力。

生物活性

MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a K i of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.

性状

Solid

IC50 & Target[1][2]

p38α 101 nM (Ki)

体外研究(In Vitro)

MW-150 inhibits in a concentration-dependent manner the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
MW-150 blocks in a concentration-dependent manner the increased IL-1β production by activated glia. The IC50 values are 332 nM and 936 nM for MK2 and IL-1β, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

MW-150 (2.5 mg/kg; oral daily for 3-4 months) improves the APP/PS1 transgenic (Tg) mice performance in radial arm water maze (RAWM) and contextual fear conditioning tests.
MW-150 (2.5 mg/kg; given i.p.; daily for 14 days) treatment in APP × PS knock-in mouse (with no overexpression of the amyloid precursor protein) exhibits RAWM behavior indistinguishable from WT 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

ClinicalTrial

参考文献

[1]. Roy SM, et al. Targeting human central nervous system protein kinases: An isoform selective p38αMAPK inhibitor that attenuates disease progression in Alzheimers disease mouse models. ACS Chem Neurosci. 2015 Apr 15;6(4):666-80.

溶解度数据	In Vitro: DMSO : 40 mg/mL (104.86 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

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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