RG3039

Product Name: RG3039
CAS No.: 1005504-62-0
Chemical Name: RG3039
Synonyms: RG3039;CS-2207;EOS-62326;EOS-61154;PF-6687859;PF-6687859 Free;RG-3039; RG3039;RG3039(PF-06687859);PF-06687859/R -3039;Rg3039, 10 mM in DMSO
CBNumber: CB72745524
Molecular Formula: C21H23Cl2N5O
Formula Weight: 432.35
MOL File: 1005504-62-0.mol

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RG3039 Property

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
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)
InChIKey: MNLHFGXIUJNDAF-UHFFFAOYSA-N
SMILES: NC1=NC(N)=C2C(OCC3CCN(CC3)CC4=C(C=CC=C4Cl)Cl)=CC=CC2=N1

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Safety

WGK Germany: WGK 3
Storage Class: 11 - Combustible Solids

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML3071
Product name: RG3039
Purity: ≥98% (HPLC)
Packaging: 5 mg
Price: $73.24
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML3071
Product name: RG3039
Purity: ≥98% (HPLC)
Packaging: 25 mg
Price: $315
Updated: 2025/07/31

DC Chemicals

Product number: DC7551
Product name: RG3039(PF-06687859)
Purity: >98%
Packaging: 100mg
Price: $500
Updated: 2021/12/16

Crysdot

Product number: CD11369359
Product name: RG3039(PF-06687859)
Purity: 95+%
Packaging: 100mg
Price: $520
Updated: 2021/12/16

DC Chemicals

Product number: DC7551
Product name: RG3039(PF-06687859)
Purity: >98%
Packaging: 250mg
Price: $1000
Updated: 2021/12/16

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RG3039 Chemical Properties,Usage,Production

Uses

RG3039 (PF-06687859) is an orally bioavailable and brain-penetrant DcpS inhibitor with an IC50 of 0.069 nM.

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 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).

in vivo

RG3039 can extend survival and improve function in two SMA mouse models of varying disease severity (Taiwanese 5058 Hemi and 2B/ SMA mice), and positively impacts neuromuscular pathologies. In 2B/ SMA mice, RG3039 provides a >600% survival benefit (median 18 days to >112 days) when dosing began at P4, highlighting the importance of early intervention^[2]. RG3039 distributes to central nervous system tissues where it robustly inhibits DcpS enzyme activity, but minimally activates SMN expression or the assembly of small nuclear ribonucleoproteins. RG3039 treated SMA mice shows a dose-dependent increase in survival, weight and motor function and it is associated with improved motor neuron somal and neuromuscular junction synaptic innervation and function and increased muscle size. RG3039 also enhances survival of conditional SMA mice^[3].

References

[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. DOI:10.1021/acs.jmedchem.7b00124
[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. DOI:10.1093/hmg/ddt258
[3] Van Meerbeke J, et al. The DcpS inhibitor RG3039 improves motor function in SMA mice. Hum Mol Genet. 2013 Oct 15;22(20):4074-83. DOI:10.1093/hmg/ddt257

RG3039 Preparation Products And Raw materials

Raw materials

Preparation Products

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RG3039 Suppliers

China 63 United States 8 Global 71

Shanghai Boyle Chemical Co., Ltd.

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MedChemexpress LLC

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AdooQ Bioscience CHINA

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Shanghai Lollane Biological Technology Co.,Ltd.

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Nanjing Chempioneer Pharmaceutical Co., Ltd.

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Wuhu Nuowei Chemical Technology Co., Ltd

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Shanghai YuanYe Biotechnology Co., Ltd.

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Tianjin Kailiqi Biotechnology Co., Ltd.

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Jinan elephant international trading co., LTD

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Shanghai Chaolan Chemical Technology Center

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1005504-62-0, RG3039Related Search:

Xylene

RG3039

RG3039(PF-06687859)

5-[[1-(2,6-Dichlorobenzyl)piperidin-4-yl]methoxy]quinazoline-2,4-diamine

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

PF-6687859

EOS-61154

EOS-62326

RG-3039; RG3039

CS-2207

2,4-Quinazolinediamine, 5-[[1-[(2,6-dichlorophenyl)methyl]-4-piperidinyl]methoxy]-

PF-6687859 Free

PF06687859,Inhibitor,PF 06687859,inhibit,Rg-3039,RG 3039,Rg3039

PF-06687859/R -3039

Rg3039, 10 mM in DMSO

1005504-62-0