(R)-氟比洛芬
中文名称 | (R)-氟比洛芬 |
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中文同义词 | (R)-(-)-2-氟-Α-甲基-4-联苯乙酸;(R)-氟比洛芬;(R)-2-氟比洛芬;氟比洛芬;(R)-(-)-2-氟-ALPHA-甲基-4-联苯乙酸;氟比洛芬 EP标准品;(R)-(-)-2-氟-Α-甲基-4-联苯乙酸;氟比洛芬15 |
英文名称 | (R)-2-Flurbiprofen |
英文同义词 | (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 (Flurbiprofe;[1,1'-Biphenyl]-4-aceticacid, 2-fluoro-a-Methyl-,(aR)-;MPC 7869;(R)-(-)-2-Fluoro-alpha-methyl-4-biphenylacetic acid 97%;(R)-Flurbiprofen, >=99%;(R)-2-Flurbiprofenr |
CAS号 | 51543-40-9 |
分子式 | C15H13FO2 |
分子量 | 244.26 |
EINECS号 | 257-264-7 |
相关类别 | 含硫化合物;医药原料;原料药;化合物:原料药;中间体;医药化工类;医药原料-抗真菌;科研试剂;API;Pharmaceutical ingredients;杂质对照品;药物杂质及中间体;原料;化学试剂-科研试剂;医药原料药;化学试剂;对照品 |
Mol文件 | 51543-40-9.mol |
结构式 |
(R)-氟比洛芬 性质
熔点 | 110-113 °C(lit.) |
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沸点 | 376.2±30.0 °C(Predicted) |
密度 | 1.199±0.06 g/cm3(Predicted) |
储存条件 | Store at RT |
溶解度 | DMF:25mg/mL; DMSO:10mg/mL;乙醇:25mg/mL; PBS(pH 7.2):0.9 mg/mL |
酸度系数(pKa) | 4.14±0.10(Predicted) |
形态 | 结晶粉末 |
颜色 | 白色至类白色 |
其他不良反应有恶心、腹泻、腹痛、视力模糊、尿路感染征候、皮炎等。少数有肝转氨酶增高,继续用药,可能发展,亦可保持不变或消失。滴入眼时有轻度的刺痛感和烧灼感及(或)视觉紊乱。因影响血小板聚集而延长出血时间,有眼科手术应用本药后增加眼内出血倾向的报道。动物实验中,氟比洛芬50~100 mg/kg,用药3月,可引起肾乳头坏死。对人类亦可有此作用。Tarenflurbil ((R)-Flurbiprofen) 是 Flurbiprofen 的 R 型对映体,Tarenflurbil ((R)-Flurbiprofen) 抑制 [3H]9-cis-RA 结合到 RXRα LBD,IC50 为 75 μM。
IC50: 75 μM (RXRα)
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.
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).
安全信息
危险品标志 | T |
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危险类别码 | 25 |
安全说明 | 26-36/37/39-45 |
危险品运输编号 | UN 2811 6.1/PG 2 |
WGK Germany | 3 |
海关编码 | 29163900 |
提供商 | 语言 |
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英文
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-10291 | (R)-氟比洛芬 Tarenflurbil | 51543-40-9 | 100mg | 550元 |
2024/04/30 | HY-10291 | (R)-氟比洛芬 Tarenflurbil | 51543-40-9 | 10mM * 1mLin DMSO | 605元 |