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Tarenflurbil ((R)-Flurbiprofen) 是 Flurbiprofen 的 R 型对映体,可抑制 [3H]9-cis-RA 结合到 RXRαLBD,IC50为 75 μM。它可研究阿尔兹海默症。
Tarenflurbil ((R)-Flurbiprofen) 是 Flurbiprofen 的 R 型对映体,可抑制 [3H]9-cis-RA 结合到 RXRαLBD,IC50为 75 μM。它可研究阿尔兹海默症。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50 mg | ¥ 327 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 497 | 现货 |
产品描述 | Tarenflurbil ((R)-Flurbiprofen) is the non-cyclooxygenase inhibiting R-enantiomer of the non-steroidal anti-inflammatory drug flurbiprofen, which was assessed as a remedy for Alzheimer's disease. |
靶点活性 | RXRα:75 μM |
体内活性 | Oral R-flurbiprofen prevented and attenuated primary progressive EAE in C57BL6/J mice and relapsing-remitting EAE in SJL mice, even if the treatment was initiated on or after the first flare of the disease.?R-flurbiprofen reduced immune cell infiltration and microglia activation and inflammation in the spinal cord, brain and optic nerve and attenuated myelin destruction and EAE-evoked hyperalgesia.?R-flurbiprofen treatment increased CD4(+)CD25(+)FoxP3(+) regulatory T cells, CTLA4(+) inhibitory T cells and interleukin-10, whereas the EAE-evoked upregulation of pro-inflammatory genes in the spinal cord was strongly reduced.?The effects were associated with an increase of plasma and cortical endocannabinoids but decreased spinal prostaglandins, the latter likely due to R to S inversion. |
动物实验 | Bone marrow transplantation (BMX), recipient C57BL6/J mice received a 9.5 Gy cobalt 60 gamma irradiation and subsequently an intravenous injection through the tail vein of 6 × 10^6 bone marrow cells, which were harvested from tibia and femur of β-actin-EGFP donor mice.?Immunization was done with MOG35-55/CFA emulsion plus PTX 3 weeks after BMX and treatment with R-flurbiprofen or vehicle started 3 days after immunization. |
别名 | 氟比洛芬, R-氟比洛芬, R-flurbiprofen, MPC7869, (R)-Flurbiprofen |
分子量 | 244.26 |
分子式 | C15H13FO2 |
CAS No. | 51543-40-9 |
Smiles | C[C@@H](C(O)=O)c1ccc(c(F)c1)-c1ccccc1 |
密度 | 1.199 g/cm3 |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (204.70 mM) | |||||||||||||||||||||||||||||||||||
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