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SB225002

Cat. No. M3887
SB225002 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 45  USD50 In stock
10mg USD 63  USD70 In stock
25mg USD 139.5  USD155 In stock
50mg USD 252  USD280 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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).
Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 352.14
Formula C13H10BrN3O4
CAS Number 182498-32-4
Purity >98%
Solubility DMSO 35 mg/mL
Storage at -20°C
References

A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer.
Wang B, et al. Cancer Res. 2006 Mar 15;66(6):3071-7. PMID: 16540656.

Characterization of the molecular interactions of interleukin-8 (CXCL8), growth related oncogen alpha (CXCL1) and a non-peptide antagonist (SB 225002) with the human CXCR2.
Catusse J, et al. Biochem Pharmacol. 2003 Mar 1;65(5):813-21. PMID: 12628493.

Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration.
White JR, et al. J Biol Chem. 1998 Apr 24;273(17):10095-8. PMID: 9553055.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SB225002 supplier, CXCR, inhibitors

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