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RG3039

Chemical Structure : RG3039

CAS No.: 1005504-62-0

RG3039 (PF-06687859)

货号: PC-47085Not For Human Use, Lab Use Only.

RG3039 (PF-06687859) is a potent, orally bioavailable and brain-penetrant inhibitor of the ribonucleic acid scavenger enzyme DcpS with IC50 of 3.4 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RG3039 (PF-06687859) is a potent, orally bioavailable and brain-penetrant inhibitor of the ribonucleic acid scavenger enzyme DcpS with IC50 of 3.4 nM.
RG3039 crosses the blood brain barrier and inhibits the RNA decapping enzyme DcpS in the CNS.
RG3039 showed a dose-dependent increase in survival, weight and motor function in SMA mice, with improved motor neuron somal and neuromuscular junction synaptic innervation and function and increased muscle size.
RG3039 also enhanced survival of conditional SMA mice in which SMN had been genetically restored to motor neurons.

物理化学性质&存储条件

分子量 432.35
分子式 C21H23Cl2N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-((1-(2,6-dichlorobenzyl)piperidin-4-yl)methoxy)quinazoline-2,4-diamine

参考文献

1. Van Meerbeke JP, et al. Hum Mol Genet. 2013 Oct 15;22(20):4074-83.

2. Gogliotti RG, et al. Hum Mol Genet. 2013 Oct 15;22(20):4084-101.

3. Calder AN, et al. J Med Chem. 2016 Nov 23;59(22):10067-10083.

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