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Rg3039
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Catalog No. T3336Cas No. 1005504-62-0
Alias PF-06687859
Rg3039 (PF-06687859) is a potent DcpS inhibitor. DcpS is a therapeutic target for spinal muscular atrophy. Spinal muscular atrophy (SMA) is caused by deletion or mutation of both copies of the SMN1 gene which produces an essential protein known as SMN. RG3039 improves motor function in SMA mice. RG3039 also showed activity to improve survival, function and motor unit pathologies in two SMA mouse models.
Rg3039
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Purity: 99.58%
Catalog No. T3336Alias PF-06687859Cas No. 1005504-62-0
Rg3039 (PF-06687859) is a potent DcpS inhibitor. DcpS is a therapeutic target for spinal muscular atrophy. Spinal muscular atrophy (SMA) is caused by deletion or mutation of both copies of the SMN1 gene which produces an essential protein known as SMN. RG3039 improves motor function in SMA mice. RG3039 also showed activity to improve survival, function and motor unit pathologies in two SMA mouse models.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $32 | In Stock | In Stock | |
| 5 mg | $51 | In Stock | In Stock | |
| 10 mg | $84 | In Stock | In Stock | |
| 25 mg | $165 | In Stock | In Stock | |
| 50 mg | $272 | In Stock | In Stock | |
| 100 mg | $438 | In Stock | In Stock | |
| 500 mg | $985 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.58%
Appearance:Solid
Color:White
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Product Introduction
Rg3039 AI Summary
Rg3039 exhibits potent inhibition of human DcpS with an IC50 of 0.069 nM, indicating potential as a therapeutic agent for increasing SMN2 promoter activity. It also shows an IC50 of 4.2 nM for the same enzyme and demonstrates significant brain distribution in the spinal muscular atrophy mouse model, with an AUC of 6762.0 ng.hr.mL-1 and a high brain to plasma ratio of 16.0. The compound's pharmacokinetic profile includes high intrinsic clearance in human liver microsomes (> 250.0 mL.min-1.g-1), good passive cell permeability, and a high efflux ratio in MDR1-expressing cells. It has a log D value of 2.8 at pH 7.4 and high kinetic solubility at pH 6.5. Although it shows good stability in human liver microsomes with a stability of 3.0 minutes at 1 uM, it also exhibits moderate cytotoxicity against human HepG2 cells with an IC50 value of 4000.0 nM.
In terms of antiviral activity, Rg3039 inhibits SARS-CoV-2 3CL-Pro protease activity by 13.4% at a concentration of 20μM and shows antiviral effects in VERO-6 cells at 10 uM concentration with an inhibition rate of -0.33% after 48 hours of exposure. The compound's efficacy and activity in the spinal muscular atrophy mouse model vary, demonstrating survival rates ranging from 26.0% to 90.0% depending on dosing and administration routes..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Rg3039 (PF-06687859) is a potent DcpS inhibitor. DcpS is a therapeutic target for spinal muscular atrophy. Spinal muscular atrophy (SMA) is caused by deletion or mutation of both copies of the SMN1 gene which produces an essential protein known as SMN. RG3039 improves motor function in SMA mice. RG3039 also showed activity to improve survival, function and motor unit pathologies in two SMA mouse models. |
| Targets&IC50 | DcpS:0.069 nM. |
| Synonyms | PF-06687859 |
| Molecular Weight | 432.35 |
| Formula | C21H23Cl2N5O |
| Cas No. | 1005504-62-0 |
| Smiles | Nc1nc(N)c2c(OCC3CCN(Cc4c(Cl)cccc4Cl)CC3)cccc2n1 |
| Relative Density. | 1.375 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||
| Solubility Information | H2O: < 0.1 mg/mL (insoluble) DMSO: 2.69 mg/mL (6.22 mM), Sonication is recommended.  | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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