Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Reparixin L-lysine salt (Repertaxin L-lysine salt) 是趋化因子受体1/2 活化的变构抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 449 | 现货 | ||
2 mg | ¥ 655 | 现货 | ||
5 mg | ¥ 1,330 | 现货 | ||
10 mg | ¥ 2,230 | 现货 | ||
25 mg | ¥ 3,780 | 现货 | ||
50 mg | ¥ 5,450 | 现货 | ||
100 mg | ¥ 7,660 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,290 | 现货 |
产品描述 | Reparixin L-lysine salt (Repertaxin L-lysine salt) is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor. |
靶点活性 | CXCR1:1 nM (in cells), CXCR1:5.6 nM (CXCR1wt, in L1.2 cells), CXCR1:80 nM (CXCR1Ile43Val; in L1.2 cells), CXCR2:100 nM (in cells) |
体外活性 | 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]. |
体内活性 | 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]. |
别名 | REPERTAXIN L-赖氨酸盐, Repertaxin L-lysine salt |
分子量 | 429.57 |
分子式 | C20H35N3O5S |
CAS No. | 266359-93-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 99 mg/mL (230.46 mM), sonification is recommended.
DMSO: 99 mg/mL (230.46 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 2.3279 mL | 11.6395 mL | 23.2791 mL | 58.1977 mL |
5 mM | 0.4656 mL | 2.3279 mL | 4.6558 mL | 11.6395 mL | |
10 mM | 0.2328 mL | 1.164 mL | 2.3279 mL | 5.8198 mL | |
20 mM | 0.1164 mL | 0.582 mL | 1.164 mL | 2.9099 mL | |
50 mM | 0.0466 mL | 0.2328 mL | 0.4656 mL | 1.164 mL | |
100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.582 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Reparixin L-lysine salt 266359-93-7 Autophagy GPCR/G Protein Immunology/Inflammation CXCR Repertaxin REPERTAXIN L-赖氨酸盐 Reparixin L-lysine inhibit Reparixin Llysine salt Reparixin L lysine salt Repertaxin L-lysine Inhibitor Reparixin Repertaxin L-lysine salt CXC chemokine receptors inhibitor