Reparixin L-lysine salt

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Reparixin L-lysine salt 是一种变构趋化因子受体 1/2 (CXCR1/2) 激活抑制剂。

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

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 (IC50 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 [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).

Repertaxin L-lysine salt

Autophagy

CXCR

CXCR1wt|CXCR1Ile43Val|CXCR1|CXCR2

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266359-93-7

429.57

C20H35N3O5S

>98% (HPLC)

H2O: 99 mg/mL (230.46 mM; Need ultrasonic); DMSO: 99 mg/mL (230.46 mM; Need ultrasonic)

N[C@@H](CCCCN)C(O)=O.O=C(NS(=O)(C)=O)[C@@H](C)C1=CC=C(CC(C)C)C=C1

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(-20℃)

With Ice Pack

≥ 2 years