266359-93-7
266359-93-7 结构式
基本信息
REPERTAXIN L-赖氨酸盐
REPERTAXIN L-LYSINE SALT
Reparixin (L-lysine salt)
Reparixin L-lysine salt (Repertaxin L-lysine salt)
R-(-)-2-(4-ISOBUTYLPHENYL)PROPIONYL METHANSULPHONAMIDE, LYSINE SALT
物理化学性质
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-15252 | REPERTAXIN L-赖氨酸盐 Reparixin L-lysine salt | 266359-93-7 | 2mg | 790元 |
| 2024/04/30 | HY-15252 | REPERTAXIN L-赖氨酸盐 Reparixin L-lysine salt | 266359-93-7 | 5mg | 1600元 |
| 2024/04/30 | HY-15252 | REPERTAXIN L-赖氨酸盐 Reparixin L-lysine salt | 266359-93-7 | 10mM * 1mLin DMSO | 1760元 |
常见问题列表
|
CXCR1 wt 5.6 nM (IC 50 , in L1.2 cells) |
CXCR1 Ile43Val 80 nM (IC 50 , in L1.2 cells) |
CXCR1 1 nM (IC 50 , in cells) |
CXCR2 ∼100 nM (IC 50 , in cells) |
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.
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).