R-氟比洛芬 T5843

Product Introduction
Bioactivity


英文名: Tarenflurbil

描述: 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。

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.

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.

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (204.70 mM)


关键字: Retinoic acid receptors | Flurbiprofen | Retinoid X receptors | Inhibitor | Tarenflurbil | MPC 7869 | RAR/RXR | inhibit | Autophagy | MPC-7869

相关产品: Retinoic acid-d5 | AGN 196996 | CD3254 | BMS 195614 | BMS453 | AC-261066 | AGN 194310 | Bexarotene | HX 531 | CD 1530

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Differentiation Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Nuclear Receptor Compound Library | NO PAINS Compound Library | Anti-Alzheimer's Disease Compound Library | Bioactive Compound Library

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