GNE-7915-tosylate - LRRK2 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGNE-7915 tosylateCat. No.: HY-18163ACAS No.: 2070015-00-6分式: CHFNOS分量: 615.6作靶點(diǎn): LRRK2作通路: Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (81.22 mM)H2O : 40% PEG300 5% Tw

2、een-80 45% salineSolubility: 2.5 mg/mL (4.06 mM); Suspended solution; Need ultrasonic2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.06 mM); Suspended solution; Need ultrasonic1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.

3、5 mg/mL (4.06 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 GNE-7915 tosylate效選擇性，可滲透腦的LRRK2抑制劑，IC50值為9 nM。IC50 & Target IC50: 9 nM 1 (LRRK2)體外研究 Maintaining the methoxy/fluoro arrangement at C-2/C-5 and varying aminoalkyl R1 substitution resultes insingle-digit nanomolar LRRK2 cellular activities for G

4、NE-7915 and compound 19. Expanded Invitrogenkinase profiling (187 kinases) at 0.1 M for both GNE-7915 (100-fold over LRRK2 Ki) and 19 (250-fold overLRRK2 Ki) resultes in only TTK showing greater than 50% inhibition. Selectivity profiling using the DiscoverXKinomeScan55 competitive binding assay pane

5、l, which includes 392 unique kinases, is also performed forGNE-7915 at 0.1 M. Binding of 50% probe displacement is detected for 10 kinases and of 65% for onlyLRRK2, TTK, and ALK, further supporting the excellent LRRK2 selectivity for GNE-7915. Cerep receptorprofiling, including expanded brain panels

6、, suggestes that GNE-7915 and 19 only inhibite 5-HT2B with 70%inhibition at 10 M. GNE-7915 and 19 are confirmed to be moderately potent 5-HT2B antagonists in vitrofunctional assays 2.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Hum Mol Genet. 2017 Jul 15;26(14):2747-2767. Programa Oficial de Doctorado en Biomedicina. Universidad de

7、 Granada. 5-Jul-2017. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Kavanagh ME, et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med ChemLett.?2013 Jul 1;23(13):3690-6.2. Estrada AA, et al. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small moleculeinhibitors. J Med Chem. 2012 Nov 26;55(22):9416-33.McePdfHeightCaution: Product has not been fully validated for medical applications.For re