Neflamapimod|209410-46-8|-陌孚医药/Medlife

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Neflamapimod

目录号: PL08732 纯度: ≥99%

CAS No. :209410-46-8

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中文名称	Neflamapimod
中文别名	5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-b]哒嗪-6-酮;4-肼基-N-甲基苯基乙烷磺酰胺盐酸盐;VX745 抑制剂
英文名称	Neflamapimod
英文别名	5-(2,6-Dichlorophenyl)-2-((2,4-difluorophenyl)thio)-6H-pyrimido[1,6-b]pyridazin-6-one;5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenyl)sulfanylpyridazino[6,1-f]pyrimidin-6-one;VX-745;5-(2,6-Dichlorophenyl)-2-((2,4-difluorophenyl)thio)-6H-pyrimido(1,6-b)pyridazin-6-one;5-(2,6-Dichlorophenyl)-2-((2,4-difluorophenyl)-thio)-6H-pyrimido[1,6-b]pyridazin-6-one;5-(2,6-dichlorophenyl)-2-(2,4-difluorophenyl)sulfanylpyrimido[1,6-b]pyridazin-6-one;6H-PYRIMIDO[1,6-B]PYRIDAZIN-6-ONE, 5-(2,6-DICHLOROPHENYL)-2-[(2,4-DIFLUOROPHENYL)THIO]- (9CI);6H-Pyrimido[1,6-b]pyridazin-6-one,5-(2,6-dichlorophenyl)-2-[(2,4-difluorophenyl)thio]-;VX 745;5-(2,6-Dichlorophenyl)-2-(2,4-difluorophenylthio)-6H-pyrimido[1,6-b]pyridazin-6-one;Neflamapimod;VX745;TYL52QM320;Neflamapimod [USAN];Neflamapimod (USAN);C19H9Cl2F2N3OS;6H-Pyrimido[1,6-b]pyridazin-6-one, 5-(2,6-dichlorophenyl)-2-[(2,4-difluorophenyl)thio]-
Cas No.	209410-46-8
分子式	C₁₉H₉Cl₂F₂N₃Os
分子量	436.26
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Neflamapimod (VX-745) 是有效的，可穿过血脑屏障的，高选择性的 p38α 抑制剂，对 p38α 的 IC₅₀ 值为 10 nM，p38β 的 IC₅₀ 值为 220 nM。Neflamapimod (VX-745) 具有抗炎活性。

生物活性

Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC 50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.

性状

Solid

IC50 & Target[1][2]

p38α 10 nM (IC50) p38β 220 nM (IC50

体外研究(In Vitro)

Neflamapimod (VX-745) exhibits PBMC IL-1β and TNFα IC50 values of 45 and 51 nM, respectively. Neflamapimod is also effective in whole blood, blocking IL-1β and TNFα release with IC50 values of 150 and 180 nM, respectively.
Neflamapimod shows a promising selectivity profile, with 20-fold selectivity for p38α over p38β (Ki=220 nM).
Neflamapimod (VX-745) solutions in DMSO/DMEM inhibits the IL-6 production with IC50 of 15±9 nM.
Neflamapimod (VX-745; 5.0 nM) displays potent activity and 1000-fold selectivity over closely related kinases, including ERK1, JNK1-3 and MK2. Neflamapimod (10 nM-50 μM) increasingly inhibits the anisomycin-induced activity of p38α.
Neflamapimod (VX-745; 0.06 μM-20 μM) inhibits IL-6 and VEGF secretion in BMSCs. Neflamapimod can inhibit cytokine (TNF-α, IL-6, VEGF)-induced paracrine MM cell growth,

体内研究(In Vivo)

Neflamapimod (VX-745; 2.5, 5, and 10 mg/kg) improves the inflammatory scores in mice by 27%, 31%, and 44%, respectively. Neflamapimod (VX-745; 1.06 mg/kg) significantly decreases the inflammation score from 2.07±0.29 for the control group to 1.42±0.06. 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]. Duffy JP, et al. The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor. ACS Med Chem Lett. 2011 Jul 28;2(10):758-63.
[2]. Cicenas J, et al. JNK, p38, ERK, and SGK1 Inhibitors in Cancer. Cancers (Basel). 2017 Dec 21;10(1).
[3]. Pradal J, et al. Intra-articular bioactivity of a p38 MAPK inhibitor a

溶解度数据	In Vitro: DMSO : 13.08 mg/mL (29.98 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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