[CAS NO. 1215493-56-3]  RG2833 (RGFP109)

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PRODUCTS SPECIFICATIONS [1215493-56-3]

Store
Catalog
SLK-S7292
Brand
Selleck
CAS
1215493-56-3

DESCRIPTION [1215493-56-3]

Overview

MDLMFCD25976845
Molecular Weight339.43
Molecular FormulaC20H25N3O2
SMILESO=C(NCCCCCC(NC1=CC=CC=C1N)=O)C2=CC=C(C)C=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.9461 mL14.7306 mL29.4612 mL
5 mM0.5892 mL2.9461 mL5.8922 mL
10 mM0.2946 mL1.4731 mL2.9461 mL
50 mM0.0589 mL0.2946 mL0.5892 mL

Description

RG2833 (RGFP109) is a brain-penetrant inhibitor with 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.

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. RGFP109 ameliorates the disease phenotype of a Friedreich ataxia mouse model. RGFP109 (30 mg/kg p.o.) also alleviates established l-DOPA-induced dyskinesia.