Reparixin L-lysine
Reparixin (L-lysine salt)
CAS: 266359-93-7
Molecular Formula: C20H35N3O5S
Reparixin L-lysine - Names and Identifiers
Reparixin L-lysine - Physico-chemical Properties
| Molecular Formula | C20H35N3O5S |
| Molar Mass | 429.57 |
| Solubility | H2O: ≥ 200 mg/mL |
| Appearance | lyophilized powder |
| Storage Condition | 2-8°C |
| In vitro study | 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. |
| In vivo study | 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). |
Reparixin L-lysine - Risk and Safety
| WGK Germany | 3 |
Reparixin L-lysine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.328 ml | 11.639 ml | 23.279 ml |
| 5 mM | 0.466 ml | 2.328 ml | 4.656 ml |
| 10 mM | 0.233 ml | 1.164 ml | 2.328 ml |
| 5 mM | 0.047 ml | 0.233 ml | 0.466 ml |
Last Update：2024-01-02 23:10:35
Reparixin L-lysine - Reference Information
| biological activity | Reparixin L-lysine salt is an allosteric inhibitor activated by chemokine receptor 1/2 (CXCR1/2). |
| target | 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) |
| in vitro study | 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. |
| in vivo study | 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 50g/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 rat (t 1/2~0.5 h) than in dogs (t 1/2~10 h). |
Last Update：2024-04-09 02:00:00
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Product Name: Reparixin (L-lysine salt) Visit Supplier Webpage Request for quotation
CAS: 266359-93-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 266359-93-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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