产品说明书
RG-2833
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同义名 : | - |
| CAS号 : | 1215493-56-3 | |
| 货号 : | A327170 | |
| 分子式 : | C20H25N3O2 | |
| 纯度 : | 98% | |
| 分子量 : | 339.431 | |
| MDL号 : | - | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(147.31 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
IP 2% DMSO+2% Tween80+30% PEG300+water 9 mg/mL clear PO 0.5% CMC-Na 37 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | A few studies find that abnormal histone deacetylation may play a role in the dyskinetic phenotype or Friedreich’s Ataxia. RG2833, also called as RGFP109, is an HDAC1/3 inhibitor with IC50 value of 60nM and 50nM (measured by purified recombinant HDAC enzymes), respectively[1]. RG2833 mainly used in the research of dyskinetic phenotype is partially due to its BBB penetration. ChIP analysis showed increased level of the acetylated H3K9, H4K5 residues within the FXN locus of brain tissue from YG8R FRDA mice (Friedreich ataxia model) given subcutaneous injections of 100mg/kg RGFP109 five times per week for 5 months. Meanwhile, a 2.6-fold increase in frataxin expression of brain tissue and the improved locomotor activity can also be observed in YG8R FRDA mice compared with control[2]. Another study show that though 30mg/kg orally treatment of RGFP109 for 6 days had no acute effect on dyskinesia of the parkinsonian marmoset, one week following cessation of RGFP109, dyskinesia and duration of ON-time with disabling dyskinesia were reduced by 37% and 50%, respectively, compared with L-DOPA alone[3]. | ||
| 作用机制 | The ortho-aminoanilide structure of RG2833 is the zinc-binding moiety. [4] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.95mL 0.59mL 0.29mL |
14.73mL 2.95mL 1.47mL |
29.46mL 5.89mL 2.95mL |
