SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM and >150-fold selectivity over CXCR1 and four other 7-TMRs. SB225002 inhibits IL-8- (IC50=8nM) and GROα-mediated (IC50=10nM) calcium mobilisation. SB225002 prevents IL-8-induced neutrophil migration. SB225002 inhibits HIV replication in lymphocytes and macrophages. SB 225002 potently inhibited human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha.
Brain Res Bull. 2017 Jul 10;134:91-98.
The effect of CXCR2 inhibition on seizure activity in the pilocarpine epilepsy mouse model
SB225002 purchased from AbMole
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Source | Brain Research Bulletin (2017). Figure 4. SB225002 (Abmole Bioscience Inc., USA) |
| Method | Western blotting | |
| Cell Lines | TLE mice | |
| Concentrations | 2 mg/kg | |
| Incubation Time | 14 consecutive days | |
| Results | To further investigate the role of CXCR2 in epilepsy, we measured the effect of SB225002 on SRSs during the chronic period in the pilocarpine-induced epilepsy mice. The latency period of SRSs was increased (by nearly 40%) in the SB225002 group as compared with the model control and vehicle groups (p < 0.05). |
| Cell Experiment | |
|---|---|
| Cell lines | WHCO1, WHCO5, and WHCO6 cell lines |
| Preparation method | Establishing three esophageal squamous cell carcinoma cell lines WHCO1, WHCO5, and WHCO6 originally from surgical biopsies of primary esophageal squamous cell carcinomas which are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2.Using the Cell Proliferation kit I to carry out MTT assays . Briefly, plating 1.5 × 103 cells in 96-well plates in a final volume of 180 μL DMEM per well.Adding SB 225002 (antagonist of CXCR2, 400 nM)to cells and adding 0.001% DMSO (solvent) as a control. After the indicated incubation period, adding 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL)to each well and incubating for 4 hours in a humidified atmosphere. Adding one hundred eighty microliters of the solubilization solution to each well and the plates were left overnight at 37°C. Using a microtiter plate reader to measure the spectrophotometric absorbance of samples at 595 nm . |
| Concentrations | 400 nM |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | Rabbits |
| Formulation | DMSO |
| Dosages | 5.5 μg/kg/min |
| Administration | Cannula in the external jugular vein |
| Molecular Weight | 352.14 |
| Formula | C13H10BrN3O4 |
| CAS Number | 182498-32-4 |
| Solubility (25°C) | DMSO ≥ 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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