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瑞帕利辛L-赖氨酸盐  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于水（100 mg/mL 超声），溶于DMSO（100 mg/mL 超声）
产品描述：基本信息 产品编号： R10319 产品名称： Reparixin L-lysine salt CAS: 266359-93-7   储存条件 粉末 -20℃ 四年     分子式： C20H35N3O5S 溶于液体 -80℃ 6个月 分子量： 429.57 -20℃ 1个月 化学名：  (2S)-2,6-diaminohexanoic acid;(2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3279mL 11.6395mL 23.2791mL 5mM 0.4656mL 2.3279mL 4.6558mL 10mM 0.2328mL 1.1640mL 2.3279mL   生物活性 产品描述 一种趋化因子受体1/2 (CXCR1/2)活化 的变构抑制剂。 靶点 CXCR   体外研究 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 (IC50 values of 5.6nM and 80nM 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. 体内研究 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 50µg/mL,but lower at higher concentrations.Although radioactivity is rapidly distributed into rat tissues,Vss is low (about 0.15L/kg) in both rat and dog.Nevertheless,Reparixin is more rapidly eliminated in rats (t1/2~0.5h) than in dogs (t1/2~10h).   推荐实验方法(仅供参考) 细胞实验:   L1.2 Cell suspension (1.5-3×106 cells/mL) is incubated at 37℃ for 15 min in the presence of vehicle or of Reparixin (1nM-1μM) and next seeded in triplicates in the upper compartment of the chemotactic chamber.Different agonists are seeded in the lower compartment of the chamber at the following concentrations:1nM CXCL8,0.03nM fMLP,10nM CXCL1,2.5nM CCL2,30nM C5a.The chemotactic chamber is incubated at 37℃ in air with 5% CO2 for 45 min (human PMNs) or 2h (monocytes).At the end of incubation,the filter is removed,fixed,and stained and five oil immersion fields at high magnification (100×) are counted for each migration well after sample coding.L1.2 migration is evaluated using 5μm pore size Transwell filters.   动物实验:   Rats and Dogs Male and female Sprague-Dawley CD (albino) rats and male Lister Hooded (partially pigmented) rats are used.Male and female beagle Dogs (age about 15 months,bodyweight range 8.3-9.4kg at the time of dosing) are used.Rats and Dogs are dosed i.v.with repurified [14C]-Reparixin free acid and an equivalent quantity of L-lysine suitably radiodiluted with Reparixin L-lysine salt in a solution of sterile isotonic (0.9%,w/v) saline. Rats are dosed with a solution of total drug concentration 9mg/mL at a dose volume of 5mL/kg (30mg free Reparixin /kg) by bolus injection into a caudal vein.Dogs are dosed with a solution of total drug concentration 100mg/mL at a dose volume of 0.5mL/kg (33mg free Reparixin/kg) by bolus injection into a superficial forelimb vein.
保存条件：-20℃

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