REPERTAXIN L-赖氨酸盐

REPERTAXIN L-赖氨酸盐

中文名称REPERTAXIN L-赖氨酸盐
中文同义词REPERTAXIN L-赖氨酸盐;瑞帕利辛L-赖氨酸盐
英文名称R-(-)-2-(4-ISOBUTYLPHENYL)PROPIONYL METHANSULPHONAMIDE, LYSINE SALT
英文同义词R-(-)-2-(4-ISOBUTYLPHENYL)PROPIONYL METHANSULPHONAMIDE, LYSINE SALT;REPERTAXIN L-LYSINE SALT;Reparixin (L-lysine salt);Reparixin L-lysine;Reparixin L-lysine salt (Repertaxin L-lysine salt);Repertaxin,CXCR,inhibit,Reparixin Llysine salt,Reparixin L lysine salt,Inhibitor,Reparixin,CXC chemokine receptors
CAS号266359-93-7
分子式C20H35N3O5S
分子量429.58
EINECS号
相关类别
Mol文件266359-93-7.mol
结构式REPERTAXIN L-赖氨酸盐 结构式

REPERTAXIN L-赖氨酸盐 性质

储存条件2-8°C
溶解度H2O: 52 mg/mL
形态冻干粉

REPERTAXIN L-赖氨酸盐 用途与合成方法

Reparixin L-lysine salt是趋化因子受体1/2 (CXCR1/2)活化 的变构抑制剂。

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).

安全信息

WGK Germany3

MSDS信息

提供商 语言
英文
更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-15252REPERTAXIN L-赖氨酸盐
Reparixin L-lysine salt
266359-93-72mg790元
2024/04/30HY-15252REPERTAXIN L-赖氨酸盐
Reparixin L-lysine salt
266359-93-75mg1600元

REPERTAXIN L-赖氨酸盐 上下游产品信息

"REPERTAXIN L-赖氨酸盐"相关产品信息
L-色氨酸 L-赖氨酸硫酸盐 REPERTAXIN
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