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RG3039 (Synonyms: PF-06687859)

Cat. No.: HY-102020 Purity: 98.36%
Handling Instructions

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

For research use only. We do not sell to patients.

RG3039 Chemical Structure

RG3039 Chemical Structure

CAS No. : 1005504-62-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
25 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 336 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 0.069 nM (DcpS)[1]

In Vitro

RG3039 is a dibasic lipophilic molecule that is predicted to accumulate in lysosomes[1]. In motor neurons, RG3039 significantly increases both the average number of cells with gems and average number of gems per cell, which is used as an indirect measure of SMN levels[2].

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 in which SMN has been genetically restored to motor neurons[3].

Solvent & Solubility
In Vitro: 

DMSO : 6 mg/mL (13.88 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3129 mL 11.5647 mL 23.1294 mL
5 mM 0.4626 mL 2.3129 mL 4.6259 mL
10 mM 0.2313 mL 1.1565 mL 2.3129 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[3]

Mice: Mice receive intraperitoneal (i.p.) injections of RG3039 starting on post natal day 1 (P1) defined as the day of birth. All treated litters are culled at P4 to a total of six pups. Daily weights and righting-time are determined starting on P1. Ambulation index is performed between P13 and P23. A compilation score is determined during two 60 s trials[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

432.35

Formula

C₂₁H₂₃Cl₂N₅O

CAS No.

1005504-62-0

SMILES

NC1=NC(N)=C2C(OCC3CCN(CC4=C(Cl)C=CC=C4Cl)CC3)=CC=CC2=N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.36%

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Product Name:
RG3039
Cat. No.:
HY-102020
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RG3039

Cat. No.: HY-102020