中文名称: SB225002  一键复制产品信息
英文名称: SB225002
CAS No: 182498-32-4
分子式: C13H10BrN3O4
分子量: 352.14
S10856 SB225002 ≥98% (普西唐-psaitong)
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
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):