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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。
中文名称:
5-[[1-(2,6-二氯苄基)哌啶-4-基]甲氧基]喹唑啉-2,4-二胺
物化属性:
PSA:91.75000
LOGP:4.19010
[1]. Gopalsamy A, et al. Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA). J Med Chem. 2017 Apr 13;60(7):3094-3108.
[2]. Gogliotti RG, et al. The DcpS inhibitor RG3039 improves survival, function and motor unit pathologies in two SMA mouse models. Hum Mol Genet. 2013 Oct 15;22(20):4084-101.
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