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RG-3039  ≥98%

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包装规格：2mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：RG3039 (PF-06687859) 是具有口服活性，可渗透大脑的 DcpS 抑制剂， IC50 值为 0.069 nM。
溶解性：溶于DMSO （5 mg/mL）
储备液保存：-80°C, 2 years -20°C, 1 year
靶点：IC50: 0.069 nM (DcpS)
体外研究：RG3039 is a dibasic lipophilic molecule that is predicted to accumulate in lysosomes. In motor neurons, RG3039 significantly increases both the average number of cells with gems and average number of gems per cell, which is used as an indirect measure of SMN levels.
体内研究：RG3039 can extend survival and improve function in two SMA mouse models of varying disease severity (Taiwanese 5058 Hemi and 2B/− SMA mice), and positively impacts neuromuscular pathologies. In 2B/− SMA mice, RG3039 provides a >600% survival benefit (median 18 days to >112 days) when dosing began at P4, highlighting the importance of early intervention. RG3039 distributes to central nervous system tissues where it robustly inhibits DcpS enzyme activity, but minimally activates SMN expression or the assembly of small nuclear ribonucleoproteins. RG3039 treated SMA mice shows a dose-dependent increase in survival, weight and motor function and it is associated with improved motor neuron somal and neuromuscular junction synaptic innervation and function and increased muscle size. RG3039 also enhances survival of conditional SMA mice in which SMN has been genetically restored to motor neurons.
保存条件：-20°C
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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