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RG3039  (Synonyms: PF-06687859)

Cat. No.: HY-102020 Purity: 99.62%
COA Handling Instructions

Molarity Calculator

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 In-stock
Solution
10 mM * 1 mL in DMSO USD 72 In-stock
Solid
5 mg USD 65 In-stock
10 mg USD 105 In-stock
25 mg USD 210 In-stock
50 mg USD 330 In-stock
100 mg USD 530 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

RG3039 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE RG3039

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

RG3039 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

432.35

Formula

C21H23Cl2N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (11.56 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.62%

COA (251 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3129 mL 11.5647 mL 23.1294 mL 57.8235 mL
5 mM 0.4626 mL 2.3129 mL 4.6259 mL 11.5647 mL
10 mM 0.2313 mL 1.1565 mL 2.3129 mL 5.7824 mL
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RG3039 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RG30391005504-62-0PF-06687859RG 3039RG-3039PF06687859PF 06687859OthersInhibitorinhibitorinhibit

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