Reparixin L-lysine salt是趋化因子受体1/2 活化的变构抑制剂。

Reparixin L-lysine salt is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor.

Reparixin is a potent CXCL8-induced inhibitor 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.Reparixin is a non-competitive allosteric inhibitor of IL-8 receptors with a 400-fold higher efficacy in inhibiting CXCR1 activity than CXCR2[2]. The efficacy of Reparixin is significantly lower in L1.2 cells expressing Ile43Val CXCR1 mutant (IC50 values of 5.6 nM and 80 nM for CXCR1 wt and CXCR1 Ile43Val, respectively)[1].

The pharmacokinetics and metabolism of Reparixin are investigated in rats and dogs after intravenous administration of [14C]-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, Vss is low (about 0.15 L/kg) in both rat and dog. Nevertheless, Reparixin is more rapidly eliminated in rats (t1/2~0.5 h) than in dogs (t1/2~10 h)[3].

266359-93-7

C20H35N3O5S

429.57

REPERTAXIN L-赖氨酸盐;Repertaxin L-lysine salt

H2O:99 mg/mL (230.46 mM),Need ultrasonic
DMSO:99 mg/mL (230.46 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years