(R)-Flurbiprofen

• CAT Number: I003858
• CAS Number: 51543-40-9
• Molecular Formula: C15H13FO2
• Molecular Weight: 244.3
• Purity: ≥95%
• Target: Gamma Secretase
• Solubility: 10 mM in DMSO
• Storage: Store at RT
• InChIKey: SYTBZMRGLBWNTM-UHFFFAOYSA-N

(R)-Flurbiprofen is the R-enantiomer of the racemate NSAID Flurbiprofen, (R)-Flurbiprofen inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM.IC50 & Target: 75 μM (RXRα)[1]InVitro: (R)-Flurbiprofen can significantly reduce Aβ secretion, but at the same time, increases the level of intracellular Aβ. The binding between [3H]9-cis-RA and RXRα is competitively inhibited by both unlabeled (R)-Flurbiprofen and 9-cis-RA. (R)-Flurbiprofen can interfere with the interaction between RXRα and 9-cis-retinoid acid (9-cis-RA), and that 9-cis-RA decreases (R)-Flurbiprofen’s reduction of Aβ secretion. (R)-Flurbiprofen treatment significantly increases the levels of intracellular Aβ species[1]. The well characterized, nonsteroidal anti-inflammatory drug (nonsteroidal anti-inflammatory drug), R-Flurbiprofen affects only Aβ and not Notch β formation, indicating that second generation GSMs and nonsteroidal anti-inflammatory drug-based GSMs have different modes of action regarding Notch processing[2].InVivo: Effects of the early and late onset of treatment with 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. 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 R-Flurbiprofen are comparable to those of Fingolimod (FTY720, 0.5 mg/kg/day), which is used as the positive control. 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)[3].

Reference

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