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GNE-7915

现货
Catalog No.
B3605
LRRK2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,120.00
现货
5mg
¥ 600.00
现货
25mg
¥ 2,000.00
现货
100mg
¥ 4,700.00
现货

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Background

GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase2 (LRRK2) inhibitor, with Ki and IC50 of 1 nM and 9 nM, respectively.
GEN-7915 is extensive inhibitor across 187 screened kinases, except TTK kinase. In an extended profile across 392 kinases, GNE-7915 only bound to 10 enzymes to a significant extent (>50% probe displaced at 100 nM). GNE-7915 and its progenitors are the first selective LRRK2 inhibitors to penetrating the brain barrier. [1]
GEN-7915 has been shown to induce dephosphorylation of LRRK2 in the brain of transgenic mice. GNE-7915 is not reported to cause cellular or genetic toxicity, and has progressed into preclinical studies in cynomolgus monkeys [3]. The use of in silico modelling, extensive in vitro assays and resource-efficient in vivo techniques to produce GNE-7915, reflects a trend towards the concerted optimisation of potency, selectivity and pharmacokinetic properties in early-stage drug development [1]. GNE-7915 can inhibit TNFαand CXCL10 at higher concentrations (≥ 3 μM) in both WT and LRRK2 KO experiments [2].
References:
1.Kavanagh ME, Doddareddy MR, Kassiou M. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3690-6. doi: 10.1016/j.bmcl.2013.04.086. Epub 2013 May 9.
2.Luerman GC, Nguyen C, Samaroo H et al. Phosphoproteomic evaluation of pharmacological inhibition of leucine-rich repeat kinase 2 reveals significant off-target effects of LRRK-2-IN-1. J Neurochem. 2014 Feb;128(4):561-76. doi: 10.1111/jnc.12483. Epub 2013 Nov 11.
3.Estrada AA, Liu X, Baker-Glenn C et al. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2012 Nov 26;55(22):9416-33. doi: 10.1021/jm301020q. Epub 2012 Oct 15.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt443.4
Cas No.1351761-44-8
FormulaC19H21F4N5O3
Solubility≥22.15mg/mL in DMSO
Chemical Name(4-((4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-2-fluoro-5-methoxyphenyl)(morpholino)methanone
SDFDownload SDF
Canonical SMILESCCNC1=C(C(F)(F)F)C=NC(NC2=CC(F)=C(C(N3CCOCC3)=O)C=C2OC)=N1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

化学结构

GNE-7915