Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Reparixin L-lysine salt (Repertaxin L-lysine salt) is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
5 mg | 在庫あり | ¥ 9,000 | |||
10 mg | 在庫あり | ¥ 13,000 | |||
25 mg | 在庫あり | ¥ 28,000 | |||
50 mg | 在庫あり | ¥ 45,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 10,000 |
説明 | Reparixin L-lysine salt (Repertaxin L-lysine salt) is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor. |
ターゲット&IC50 | 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) |
In vitro | 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]. |
In vivo | 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]. |
別名 | 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), Sonication is recommended.
DMSO: 99 mg/mL (230.46 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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