RG2833 (RGFP109)

Catalog No.S7292

For research use only.

RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively.

RG2833 (RGFP109) Chemical Structure

CAS No. 1215493-56-3

Selleck's RG2833 (RGFP109) has been cited by 14 publications

Purity & Quality Control

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Biological Activity

Description RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively.
Features Orally bioavailable, HDAC inhibitor that penetrates into brain tissue.
Targets
HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
5 nM(Ki) 32 nM(Ki)
In vitro

RGFP109 dose-dependently upregulates frataxin mRNA and protein levels in cultures of unstimulated peripheral blood mononuclear cells (PBMC) obtained from FRDA patients. [1]

In vivo RG2833 (150 mg/kg) corrects frataxin deficiency and increases histone acetylation in the brain and heart of KIKI mice without acute toxicity signs. [1] RGFP109 ameliorates the disease phenotype of a Friedreich ataxia mouse model. [2] RGFP109 (30 mg/kg p.o.) also alleviates established l-DOPA-induced dyskinesia. [3]

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: KIKI mice
  • Dosages: ~150 mg/kg
  • Administration: Subcutaneous injection

Solubility (25°C)

In vitro

DMSO 68 mg/mL
(200.33 mM)
Ethanol 10 mg/mL
(29.46 mM)
Water Insoluble

Chemical Information

Molecular Weight 339.43
Formula

C20H25N3O2

CAS No. 1215493-56-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC=C(C=C1)C(=O)NCCCCCC(=O)NC2=CC=CC=C2N

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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