GNE-7915 tosylate

A selective LRRK2 inhibitor

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5mg

￥550.00

440.00

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10mg

￥975.00

780.00

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25mg

￥1900.00

1520.00

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50mg

￥3250.00

2600.00

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100mg

￥5362.00

4290.00

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货号: ajce56584
CAS: 2070015-00-6
别名:
分子式: C26H29F4N5O6S
分子量: 615.6
纯度: >98%
溶解度: DMSO: ≥ 50 mg/mL (81.22 mM); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson's disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. GNE-7915 is a selective, brain-penetrable LRRK2 inhibitor (K_is = 2 and 18.7 nM in biochemical and cell-based assays, respectively).¹ It inhibits LRRK2 Ser¹²⁹² autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation with an IC₅₀ value of 20 nM in vivo.¹

1.Estrada, A.A., Chan, B.K., Baker-Glenn, C., et al.Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitorsJ. Med. Chem.57(3)921-936(2014)