产品说明书

RG3039

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Chemical Structure| 1005504-62-0 同义名 : PF-06687859;Quinazoline 495;PF 6687859
CAS号 : 1005504-62-0
货号 : A129874
分子式 : C21H23Cl2N5O
纯度 : 98%
分子量 : 432.346
MDL号 : MFCD28716151
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(9.25 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The human decapping scavenger enzyme (DcpS), belonging to the HIT family of pyrophosphatases, catalyzes residual cap hydrolysis following mRNA degradation and prevents accumulation of intermediates that might interfere with translation and normal processing of mRNAs[1]. RG3039 displays a potent DcpS inhibitory activity with an IC50 of 4.2 ± 0.13 nM and an IC90 of 40 nM in the DcpS inhibition assay. It shows good brain penetration with high brain-to-plasma partitioning and a half-life of ∼10 h. RG3039-treated (oral gavage with 20 mg/kg) SMA (spinal muscular atrophy) mice had a median survival that was 38% greater than vehicle-treated SMA mice[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.13mL

4.63mL

2.31mL
参考文献

[1]Gopalsamy A, Narayanan A, Liu S, 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;60(7):3094-3108

[2]Gogliotti RG, Cardona H, Singh J, et al. The DcpS inhibitor RG3039 improves survival, function and motor unit pathologies in two SMA mouse models. Hum Mol Genet. 2013;22(20):4084-4101