RG2833(RGFP109),Brain-penetrantHDACInhibitor
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產品名稱: RG2833(RGFP109),Brain-penetrantHDACInhibitor
產品型號: M60225-2s
產品展商: 其它品牌
產品文檔: 無相關文檔
簡單介紹
RG2833(RGFP109),Brain-penetrantHDACInhibitor
RG2833(RGFP109),Brain-penetrantHDACInhibitor
的詳細介紹
Product Information
| Molecular Weight: |
339.43 |
| Formula: |
C20H25N3O2
|
| Purity: |
≥98% |
| CAS#: |
1215493-56-3 |
| Solubility: |
DMSO up to 100 mM |
| Chemical Name: |
N-(6-((2-aminophenyl)amino)-6-oxohexyl)-4-methylbenzamide |
| Storage: |
Powder: 4oC 1 year.
DMSO: 4oC 3 month;
-20oC 1 year. |
Biological Activity:
RG2833 (RGFP109) is a potent and selective brain-penetrant
HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3,
respectively. It upregulates
frataxin mRNA and protein levels dose-dependently in cultures of unstimulated
peripheral blood mononuclear cells (PBMC) obtained from FRDA patients. In vivo
it corrects frataxin deficiency and increases histone acetylation in the brain
and heart of KIKI mice without acute toxicity signs.
How to Use:
In vitro:? RG2833 was used at 10 μM final concentration
in vitro and cellular assays.
In vivo: RG2833 (RGFP109) could
be dosed to KIKI mice by subcutaneous injection at 150 mg/kg, correct frataxin
deficiency and increases histone acetylation in the brain and heart of KIKI
mice without acute toxicity signs. RG2833 could be orally dosed to mice at 30 mg/kg,
alleviate established l-DOPA-induced dyskinesia.
Reference:
- 1.?????
Rai
M, et al. Two new pimelic diphenylamide HDAC inhibitors induce sustained
frataxin upregulation in cells from Friedreich's ataxia patients and in a mouse
model. (2010) PLoS One.? 5(1), e8825.
- 2.?????
Sandi
C, et al. Prolonged treatment with pimelic o-aminobenzamide HDAC inhibitors
ameliorates the disease phenotype of a Friedreich ataxia mouse model. (2011)
Neurobiol Dis. 42(3), 496-505.
- 3. ? ?Johnston TH, et al. RGFP109, a histone deacetylase inhibitor
attenuates L-DOPA-induced dyskinesia in the MPTP-lesioned marmoset: a
proof-of-concept study. (2013) Parkinsonism Relat Disord. 19(2), 260-264.
Products are for research
use only. Not for human use.?
