中文名 | Reparixin (L-lysine salt) |
英文名 | Reparixin (L-lysine salt) |
别名 | 瑞帕利辛L-赖氨酸盐 REPERTAXIN L-赖氨酸盐 |
英文别名 | Reparixin L-lysine REPERTAXIN L-LYSINE SALT Reparixin (L-lysine salt) Reparixin L-lysine salt (Repertaxin L-lysine salt) R-(-)-2-(4-ISOBUTYLPHENYL)PROPIONYL METHANSULPHONAMIDE, LYSINE SALT |
CAS | 266359-93-7 |
化学式 | C20H35N3O5S |
分子量 | 429.57 |
溶解度 | H2O: 52 mg/mL |
存储条件 | 2-8°C |
外观 | 冻干粉 |
体外研究 | Reparixin is a potent functional inhibitor of CXCL8-induced biological activities on human PMNs with a marked selectivity (around 400-fold) for CXCR1, as shown in specific experiments on CXCR1/L1.2 and CXCR2/L1.2 transfected cells and on human PMNs. The efficacy of Reparixin is significantly lower in L1.2 cells expressing Ile43Val CXCR1 mutant (IC 50 values of 5.6 nM and 80 nM for CXCR1 wt and CXCR1 Ile43Val, respectively). Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2. |
体内研究 | The pharmacokinetics and metabolism of Reparixin are investigated in rats and dogs after intravenous administration of [ 14 C]-Reparixin L-lysine salt. Plasma protein binding of Reparixin is >99% in the laboratory animals and humans up to 50 µg/mL, but lower at higher concentrations. Although radioactivity is rapidly distributed into rat tissues, V ss is low (about 0.15 L/kg) in both rat and dog. Nevertheless, Reparixin is more rapidly eliminated in rats (t 1/2 ~0.5 h) than in dogs (t 1/2 ~10 h). |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.328 ml | 11.639 ml | 23.279 ml |
5 mM | 0.466 ml | 2.328 ml | 4.656 ml |
10 mM | 0.233 ml | 1.164 ml | 2.328 ml |
5 mM | 0.047 ml | 0.233 ml | 0.466 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!