REPERTAXIN L-赖氨酸盐
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- CAS号:
- 266359-93-7
- 英文名:
- R-(-)-2-(4-ISOBUTYLPHENYL)PROPIONYL METHANSULPHONAMIDE, LYSINE SALT
- 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;Repertaxin,CXCR,inhibit,Reparixin Llysine salt,Reparixin L lysine salt,Inhibitor,Reparixin,CXC chemokine receptors
- 中文名:
- REPERTAXIN L-赖氨酸盐
- 中文别名:
- 瑞帕利辛L-赖氨酸盐;REPERTAXIN L-赖氨酸盐
- CBNumber:
- CB7461888
- 分子式:
- C20H35N3O5S
- 分子量:
- 429.58
- MOL File:
- 266359-93-7.mol
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REPERTAXIN L-赖氨酸盐化学性质
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储存条件:
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2-8°C
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溶解度:
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H2O: 52 mg/mL
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形态:
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lyophilized powder
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颜色:
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Off-white to light yellow
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REPERTAXIN L-赖氨酸盐性质、用途与生产工艺
Reparixin L-lysine salt是趋化因子受体1/2 (CXCR1/2)活化 的变构抑制剂。
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CXCR1
wt
5.6 nM (IC
50
, in L1.2 cells)
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CXCR1
Ile43Val
80 nM (IC
50
, in L1.2 cells)
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CXCR1
1 nM (IC
50
, in cells)
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CXCR2
∼100 nM (IC
50
, in cells)
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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).
REPERTAXIN L-赖氨酸盐
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
266359-93-7, REPERTAXIN L-赖氨酸盐 相关搜索:
- C20H35N3O5S
- C14H21NO3SC6H14N2O2
- 瑞帕利辛L-赖氨酸盐
- REPERTAXIN L-赖氨酸盐
- 266359-93-7
- Repertaxin,CXCR,inhibit,Reparixin Llysine salt,Reparixin L lysine salt,Inhibitor,Reparixin,CXC chemokine receptors
- Reparixin L-lysine salt (Repertaxin L-lysine salt)
- Reparixin L-lysine
- Reparixin (L-lysine salt)
- REPERTAXIN L-LYSINE SALT
- R-(-)-2-(4-ISOBUTYLPHENYL)PROPIONYL METHANSULPHONAMIDE, LYSINE SALT