中文名称: | SB225002 一键复制产品信息 | ||||
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英文名称: | SB225002 | ||||
别名: | N-(2-羟基-4-硝基苯基)-N'-(2-溴苯基)脲;1-(2-溴苯基)-3-(2-羟基-4-硝基苯基)脲 1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea;N-(2-hydroxy-4-nitrophenyl)-N'-(2-bromophenyl)urea | ||||
CAS No: | 182498-32-4 | 分子式: | C13H10BrN3O4 | 分子量: | 352.14 |
CAS No: | 182498-32-4 | ||||
分子式: | C13H10BrN3O4 | ||||
分子量: | 352.14 |
基本信息
产品编号: |
S10856 |
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产品名称: |
SB225002 |
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CAS: |
182498-32-4 |
储存条件 |
粉末 |
2-8℃(氮气保存) |
四年 |
分子式: |
溶于液体 |
-80℃(氮气保存) |
6个月 |
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分子量: |
352.14 |
-20℃(氮气保存) |
1个月 |
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化学名: |
1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea |
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Solubility (25°C): |
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体外:
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DMSO |
70mg/mL (198.78mM) |
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Ethanol |
14mg/mL warmed with 50ºC water bath (39.75mM) |
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Water |
Insoluble |
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体内(现配现用): |
2% DMSO+30% PEG 300+5% Tween 80+ddH2O |
5mg/mL |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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 |
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: |
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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: |
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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). |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )