Reparixin L-lysine salt
作者：齐岳
发布时间：2023-09-12
09:12:38
点击数：
产品名称：Reparixin L-lysine salt
产品描述：
| 产品描述 | Reparixin 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-lysine salt, REPERTAXIN L-赖氨酸盐 |
| 分子量 | 429.57 |
| 分子式 | C20H35N3O5S |
| CAS No. | 266359-93-7 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: 99 mg/mL (230.46 mM),Need ultrasonic
DMSO: 99 mg/mL (230.46 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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