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GNE-7915

Catalog No.GC12121

Potent and selective LRRK2 inhibitor

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GNE-7915 Chemical Structure

Cas No.: 1351761-44-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$83.00
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5mg
$44.00
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25mg
$153.00
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100mg
$345.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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

Cas No. 1351761-44-8 SDF
Chemical Name (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
Formula C19H21F4N5O3 M.Wt 443.4
Solubility ≥ 22.15mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.
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Average Rating: 5 ★★★★★ (Based on Reviews and 17 reference(s) in Google Scholar.)

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