RGFP 966 Datasheet DC Chemicals
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Cat.No DC7263
Name RGFP 966

Chemical Properties

CAS 1357389-11-7
Formula C21H19FN4O
MW 362.4
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological activity

Description
Target:
In Vivo RGFP966 (10 and 25 mg/kg) treatment significantly improves body weight, rotarod performance and several measures of motor function in the open field locomoter test[3]. RGFP966 at a 10 mg/kg dose penetrates the blood-brain barrier into rat auditory cortex with typical pharmacokinetics, which together establish feasibility for the modulation of A1 plasticity due to action in the auditory cortex[4].
In Vitro RGFP966 potently and selectively inhibits HDAC 3 with IC50 of 0.21 μM in RAW 264.7 macrophages, while HDACs 1 (IC50=5.6 μM), 2 (9.7 μM) and 8 (>100 μM), indicating a good level of selectivity for HDAC 3. The mRNA levels of HDACs 1, 2 and 3 are not significantly affected by RGFP966 in RAW 264.7 macrophages, whereas the HDAC 1 and HDAC 2 protein levels are slightly, though significantly, reduced upon RGFP966 treatment. Moreover, RGFP966 significantly reduced the transcriptional activity of NF-κB p65, whereas NF-κB p65 acetylation and localization remain unaltered[2].
Kinase Assay
Cell Assay
Animal Administration

References

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