| 中文名 | 氟比洛芬 |
| 英文名 | (2R)-2-(3-fluoro-4-phenyl-phenyl)propanoic acid |
| 别名 | 氟比洛芬 R-氟比洛 (R)-氟比洛芬 R(-)氟比洛芬 (R)-2-氟比洛芬 氟比洛芬 EP标准品 (R)-(-)-2-氟-Α-甲基-4-联苯乙酸 (R)-(-)-2-氟-alpha-甲基-4-联苯乙酸 (R)-(-)-2-氟-ALPHA-甲基-4-联苯乙酸 |
| 英文别名 | Flurizan MPC 7869 Flurbiprofen (R)-2-Flurbiprofen (2R)-2-(2-fluorobiphenyl-4-yl)propanoic acid (2R)-2-(3-fluoro-4-phenyl-phenyl)propanoic acid (R)-2-Fluoro-α-methyl-1,1'-biphenyl-4-acetic acid (R)-α-Methyl-2-fluoro-1,1'-biphenyl-4-acetic acid (R)-(-)-2-Fluoro-alpha-methyl-4-biphenylacetic acid 1,4-bis(1,1,1,2,3,3,3-heptafluoropropan-2-yl)benzene [1,1'-Biphenyl]-4-aceticacid, 2-fluoro-a-Methyl-,(aR)- (R)-(-)-2-Fluoro-alpha-methyl-4-biphenylacetic acid (Flurbiprofe [1,1'-biphenyl]-4-acetic acid, 2-fluoro-alpha-methyl-, (alphaR)- |
| CAS | 51543-40-9 5104-49-4 |
| EINECS | 257-264-7 |
| 化学式 | C15H13FO2 |
| 分子量 | 244.26 |
| InChI | InChI=1/C12H4F14/c13-7(9(15,16)17,10(18,19)20)5-1-2-6(4-3-5)8(14,11(21,22)23)12(24,25)26/h1-4H |
| 密度 | 1.199±0.06 g/cm3(Predicted) |
| 熔点 | 110-113°C(lit.) |
| 沸点 | 376.2±30.0 °C(Predicted) |
| 闪点 | 57.7°C |
| 蒸汽压 | 2.84mmHg at 25°C |
| 溶解度 | Soluble in DMSO (50 mg/ml), methanol (50 mg/ml), ethanol (~100 mg/ml), DMF (~100 mg/ml) |
| 折射率 | 1.34 |
| 酸度系数 | 4.14±0.10(Predicted) |
| 存储条件 | Room Temprature |
| 外观 | Crystalline Powder |
| 颜色 | White to off-white |
| MDL号 | MFCD00079303 |
| 体外研究 | Tarenflurbil ((R)-Flurbiprofen) can significantly reduce Aβ secretion, but at the same time, increases the level of intracellular Aβ. The binding between [ 3 H]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 Tarenflurbil ((R)-Flurbiprofen)’s reduction of Aβ secretion. Tarenflurbil ((R)-Flurbiprofen) treatment significantly increases the levels of intracellular Aβ species. The well characterized, nonsteroidal anti-inflammatory drug (nonsteroidal anti-inflammatory drug), Tarenflurbil ((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. |
| 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). |