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GNE-7915 Sale

目录号 : GC12121

A selective LRRK2 inhibitor

GNE-7915 Chemical Structure

Cas No.:1351761-44-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥851.00
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5mg
¥452.00
现货
25mg
¥1,565.00
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100mg
¥3,518.00
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产品描述

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

Cas No. 1351761-44-8 SDF
化学名 (4-((4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-2-fluoro-5-methoxyphenyl)(morpholino)methanone
Canonical SMILES CCNC1=C(C(F)(F)F)C=NC(NC2=CC(F)=C(C(N3CCOCC3)=O)C=C2OC)=N1
分子式 C19H21F4N5O3 分子量 443.4
溶解度 ≥ 22.15mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.2553 mL 11.2765 mL 22.553 mL
5 mM 0.4511 mL 2.2553 mL 4.5106 mL
10 mM 0.2255 mL 1.1276 mL 2.2553 mL
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