Tarenflurbil 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。
产品描述
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.
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.
Cas No.
51543-40-9
分子式
C15H13FO2
分子量
244.26
别名
MPC7869;R-氟比洛芬;氟比洛芬;(R)-Flurbiprofen;R-flurbiprofen
储存和溶解度
DMSO:50 mg/mL (204.70 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years