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SB225002  ≥98%

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包装规格：1g in glass bottle
溶解性：溶于DMSO（≥100mg/mL）
产品描述：基本信息 产品编号： S10856 产品名称： SB225002 CAS: 182498-32-4   储存条件 粉末 2-8℃(氮气保存) 四年 分子式： C13H10BrN3O4 溶于液体 -80℃(氮气保存) 6个月 分子量： 352.14 -20℃(氮气保存) 1个月 化学名：  1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea Solubility (25°C)：   体外:   DMSO 70mg/mL (198.78mM) Ethanol 14mg/mL warmed with 50ºC water bath (39.75mM) Water Insoluble 体内(现配现用): 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL ＜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 2.8398mL 14.1989mL 28.3978mL 5mM 0.5680mL 2.8398mL 5.6796mL 10mM 0.2840mL 1.4199mL 2.8398mL 50mM 0.0568mL 0.2840mL 0.5680mL   生物活性 产品描述 一种有效的选择性 CXCR2 非肽拮抗剂，抑制 125I-IL-8 和 CXCR2 结合的 IC50 为 22nM。 靶点 125I-IL-8-CXCR2 22nM (IC50,in CHO cell membrane)   体外研究 SB225002 (SB 225002) is an antagonist of 125I-IL-8 binding to CXCR2 with an IC50=22nM.SB225002 shows>150-fold selectivity over CXCR1 and four other 7-TMRs tested.SB225002 is a potent antagonist of rabbit CXCR2,inhibiting rabbit PMN chemotaxis in response to optimal concentrations of human IL-8 or GROα (IC50 values of 30 and 70nM,respectively.In these cells (PMN, HL60,CXCR1-RBL-2H3), SB225002 produces a concentration-dependent inhibition of both IL-8- and GROαmediated calcium mobilization with IC50 values of 8 and 10nM,respectively.In 3ASubE cells stably transfected with CXCR2,SB 225002 dose-dependently inhibits calcium mobilization induced by both GROα and IL-8,with IC50 values of 20 and 40nM,respectively.WHCO1 cells treated with SB225002 exhibits a 40% reduction in cell proliferation. Blocking CXCR2 signaling in WHCO1 cells with 400nM SB225002 (SB 225002) significantly decreases cell proliferation by ~40% to 50%. 体内研究 SB225002 (SB 225002) selectively blocks IL-8-induced neutrophil margination in rabbits.CXCR2 is blocked using the selective antagonist SB225002 (2mg/kg) or neutralizing CXCR2 antiserum.The CXCR2 antagonist SB225002 decreases neutrophil counts in ischemic hemispheres of ApoE−/−mice on Western diet and wildtype mice on normal diet.SB225002 significantly attenuates microglial activation and BBB damage,increases myelination,and reduces astrogliosis in the white matter after LPS-sensitized HI.   推荐实验方法(仅供参考) 激酶实验： CHO-CXCR1 and CHO-CXCR2 membranes are prepared.Assays are performed in 96-well microtiter plates where the reaction mixture contained 1.0μg/mL membrane protein in 20mM Bis-Tris-propane, pH 8.0,with 1.2mM MgSO4,0.1mM EDTA,25mM NaCl,and 0.03% CHAPS and SB 225002 (10mM stock in Me2SO) added at the indicated concentrations,the final Me2SO concentration is <1% under standard binding conditions. Binding is initiated by addition of 0.25nM 125I-IL-8 (2,200 Ci/mmol).After 1-h incubation at room temperature the plate is harvested using a Tomtec 96-well harvester onto a glass fiber filtermat blocked with 1% polyethyleneimine,0.5% BSA and washed three times with 25mM NaCl,10mM Tris•HCl,1mM MgSO4,0.5mMEDTA,0.03% CHAPS,pH 7.4.The filter is dried,sealed in a sample bag containing 10mL of Wallac 205 Betaplate liquid scintillation fluid,and counted with a Wallac 1205 Betaplate liquid scintillation counter.   细胞实验:   Three esophageal squamous cell carcinoma cell lines WHCO1,WHCO5,and WHCO6 originally established from surgical biopsies of primary esophageal squamous cell carcinomas are cultured in DMEM containing 10% FCS at 37℃ in a humidified atmosphere of 5% CO2.MTT assays are carried out using the Cell Proliferation kit.Briefly,1.5×103 cells are plated in 96-well plates in a final volume of 180μL DMEM per well.SB 225002 (400nM) is added to cells and 0.001% DMSO (solvent) is added as a control.After the indicated incubation period,18μL of the MTT labeling reagent (final concentration 0.5mg/mL) is added to each well and incubated for 4 hours in a humidified atmosphere.One hundred eighty microliters of the solubilization solution are added to each well and the plates are left overnight at 37℃.The spectrophotometric absorbance of samples is measured at 595 nm using a microtiter plate reader.   动物实验:   Rats In this study,10-12 Sprague-Dawley rat pups per dam are used.The pups receive intraperitoneal injections of SB225002 (1 or 3mg/kg,diluted in NS containing 0.33 % Tween 80) or vehicle (NS solution containing 0.33 % Tween 80) 30 min before lipopolysaccharide (LPS) administration and immediately after hypoxic ischemia (HI). The pups are randomly assigned to four groups: control (pups unexposed to LPS or HI, N=14),vehicle (NS injections 30 min before LPS administration and immediately after HI,N=18),and SB-1 (1mg/kg,N=14) and SB-3 (3mg/kg,N=18) (SB225002 injections 30 min before LPS administration and immediately after HI).
保存条件：2-8℃ 充氮保存

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