GNE-7915
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GNE-7915是高效\选择性和脑穿透性的富亮氨酸重复激酶2(LRRK2)的抑制剂,Ki值和IC50值分别为1 nM和9 nM.
GNE-7915是针对187种筛选的激酶的广谱抑制剂,除了TTK激酶.拓展到392种激酶时,GNE-7915仅显著结合10种激酶(100 nM浓度下取代超过50%的探针).GNE-7915及其前体是穿透脑屏障的第一类选择性LRRK2抑制剂[1].
GEN-7915能诱导转基因小鼠脑中LRRK2的去磷酸化.目前尚无GEN-7915具有细胞或基因毒性的报道,已在猕猴中进行临床前研究[3].通过硅片模型,大量体外研究和资源高效体内技术以生产GEN-7915,反映出在药物开发早期效应\选择性和药代动力学特性协同优化的趋势[1].在野生型和LRRK2 KO实验中,高浓度GEN-7915 (≥ 3 μM)能抑制TNFα和CXCL10[2].
参考文献:
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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 443.4 |
Cas No. | 1351761-44-8 |
Formula | C19H21F4N5O3 |
Solubility | ≥22.15 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | (4-((4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-2-fluoro-5-methoxyphenyl)(morpholino)methanone |
SDF | Download SDF |
Canonical SMILES | CCNC1=C(C(F)(F)F)C=NC(NC2=CC(F)=C(C(N3CCOCC3)=O)C=C2OC)=N1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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