| 产品描述: | Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research. |
| 靶点: |
IC50: 75 μM (RXRα);RetinoidReceptor;Autophagy |
| 体内研究: |
Effects of the early and late onset of treatment with Tarenflurbil ((R)-Flurbiprofen) are assessed in C57BL6/J mice that develop a non-remitting form of the disease, and in SJL mice that develop a relapsing-remitting (RR)-EAE. Tarenflurbil ((R)-Flurbiprofen) completely prevents the development of clinical EAE scores in C57BL6/J mice when the treatment is started within 3 days after immunization. This regimen is referred to as preventive treatment. The effect is dose-dependent, and the minimum daily dose for complete prevention is 5 mg/kg/day. Effects of Tarenflurbil ((R)-Flurbiprofen) are comparable to those of Fingolimod (FTY720, 0.5 mg/kg/day), which is used as the positive control. Tarenflurbil ((R)-Flurbiprofen) also significantly reduces clinical EAE scores in C57BL6/J mice when treatment is started shortly before onset of clinical manifestations, referred to as semi-therapeutic (10 mg/kg/day) and reduces clinical scores when the treatment is initiated after full development of the disease on day 13 (5 mg/g/day) |
| 参考文献: |
1. You X, et al. Retinoid X receptor-alpha mediates (R )-flurbiprofen's effect on the levels of Alzheimer's beta-amyloid. J Neurochem. 2009 Oct;111(1):142-9. 2. Wanngren J, et al. Second generation γ-secretase modulators exhibit different modulation of Notch β and Aβ production. J Biol Chem. 2012 Sep 21;287(39):32640-50. 3. Schmitz K, et al. R-flurbiprofen attenuates experimental autoimmune encephalomyelitis in mice. EMBO Mol Med. 2014 Sep 30;6(11):1398-422. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃;充氩 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
4.094 ml |
20.47 ml |
40.94 ml |
| 5 mM |
0.819 ml |
4.094 ml |
8.188 ml |
| 10 mM |
0.409 ml |
2.047 ml |
4.094 ml |
| 50 mM |
0.082 ml |
0.409 ml |
0.819 ml |
|
| 注意: |
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