所有图片(1)
别名:
5-[[1-(2,6-Dichlorobenzyl)piperidin-4-yl]methoxy]quinazoline-2,4-diamine, 5-[[1-[(2,6-Dichlorophenyl)methyl]-4-piperidinyl]methoxy]-2,4-quinazolinediamine, D157495, PF 06687859, PF-06687859, PF06687859, RG 3039, RG-3039
经验公式（希尔记法）:
C21H23Cl2N5O
推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
NC1=NC(N)=C2C(OCC3CCN(CC3)CC4=C(C=CC=C4Cl)Cl)=CC=CC2=N1
InChI
1S/C21H23Cl2N5O/c22-15-3-1-4-16(23)14(15)11-28-9-7-13(8-10-28)12-29-18-6-2-5-17-19(18)20(24)27-21(25)26-17/h1-6,13H,7-12H2,(H4,24,25,26,27)
InChI key
MNLHFGXIUJNDAF-UHFFFAOYSA-N
生化/生理作用
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 DcpS, respectively, 2 h & 72 h post last 3 mg/kg daily ip. from P1 to P10). In a murine severe spinal muscular atrophy (SMA) model, RG3039 (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).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Blazej A Wojtczak et al.
Journal of the American Chemical Society, 140(18), 5987-5999 (2018-04-21)
The 5' cap consists of 7-methylguanosine (m7G) linked by a 5'-5'-triphosphate bridge to messenger RNA (mRNA) and acts as the master regulator of mRNA turnover and translation initiation in eukaryotes. Cap analogues that influence mRNA translation and turnover (either as
James P Van Meerbeke et al.
Human molecular genetics, 22(20), 4074-4083 (2013-06-04)
Spinal muscular atrophy (SMA) is caused by mutations of the survival motor neuron 1 (SMN1) gene, retention of the survival motor neuron 2 (SMN2) gene and insufficient expression of full-length survival motor neuron (SMN) protein. Quinazolines increase SMN2 promoter activity
Ariamala Gopalsamy et al.
Journal of medicinal chemistry, 60(7), 3094-3108 (2017-03-04)
The C-5 substituted 2,4-diaminoquinazoline RG3039 (compound 1), a member of a chemical series that was identified and optimized using an SMN2 promoter screen, prolongs survival and improves motor function in a mouse model of spinal muscular atrophy (SMA). It is
Alyssa N Calder et al.
Journal of medicinal chemistry, 59(22), 10067-10083 (2016-08-05)
Spinal muscular atrophy (SMA) is an autosomal recessive neurodegenerative disease resulting from pathologically low levels of survival motor neuron (SMN) protein. The majority of mRNA from the SMN2 allele undergoes alternative splicing and excludes critical codons, causing an SMN protein
Rocky G Gogliotti et al.
Human molecular genetics, 22(20), 4084-4101 (2013-06-06)
Spinal muscular atrophy (SMA) is caused by insufficient levels of the survival motor neuron (SMN) protein due to the functional loss of the SMN1 gene and the inability of its paralog, SMN2, to fully compensate due to reduced exon 7
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