| Identification | Back Directory | [Name]
RG3039 | [CAS]
1005504-62-0 | [Synonyms]
RG3039
CS-2207
EOS-61154
EOS-62326
PF-6687859
RG-3039; RG3039
RG3039(PF-06687859)
5-[[1-(2,6-Dichlorobenzyl)piperidin-4-yl]methoxy]quinazoline-2,4-diamine
2,4-Quinazolinediamine, 5-[[1-[(2,6-dichlorophenyl)methyl]-4-piperidinyl]methoxy]-
5-((1-(2,6-dichlorobenzyl)piperidin-4-yl)methoxy)quinazoline-2,4-diaminedihydrochloride | [Molecular Formula]
C21H23Cl2N5O | [MDL Number]
MFCD28716151 | [MOL File]
1005504-62-0.mol | [Molecular Weight]
432.35 |
| Chemical Properties | Back Directory | [Boiling point ]
648.1±65.0 °C(Predicted) | [density ]
1.375±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:2.0(Max Conc. mg/mL);4.6(Max Conc. mM) | [form ]
A solid | [pka]
7.82±0.30(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
RG3039 is a brain-penetrant and potent inhibitor against the scavenger mRNA-decapping enzyme DcpS (m7GpppX diphosphatase) in vitro (mouse DcpS IC50 = 3.4 nM) and in mice in vivo (∼90% & ∼80% inhibition of brain DcpSrespectively2 h & 72 h post last 3 mg/kg daily ip. from P1 to P10). In a murine severe spinal muscular atrophy (SMA) modelRG3039 (10-20 mg/kg/d ip. from P1 till death) increases SMAΔ7 mice survival (by 26%) and motor function with a ∼50% increase of VGLUT1 synapses number on L3-L5 motor neurons (33.7/WT mice at P13 vs. 17.2/SMA mice without 26.1/SMA mice with RG3039 treatment). |
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