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A cell-permeable, cyclobutenedione derivative that acts as a potent antagonist of chemokine receptor CXCR2 (IL8RB) (IC50 = 8 nM). Reported to inhibit CXCR2-mediated chemotaxis in a CXCR2 expressing cell line (IC50 = 145 nM). Exhibits good stability in human and rat liver microsomal preparations (> 50% remaining after 30 min at 37°C).
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
A cell-permeable, cyclobutenedione derivative that acts as a potent antagonist of chemokine receptor CXCR2 (IL8RB) (IC50 = 8 nM). Reported to inhibit CXCR2-mediated chemotaxis in a CXCR2 expressing cell line (IC50 = 145 nM). Exhibits good stability in human and rat liver microsomal preparations (> 50% remaining after 30 min at 37°C).
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
473728-67-5
Chemical formula
C₁₈H₂₁N₃O₄
Purity
≥95% by HPLC
Solubility
DMSO (50 mg/ml; light brown solution)
Storage
Protect from light
-20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Regulatory Review
References
Merritt, J., et al. 2006. Bioorg. Med. Chem. Lett.16, 4107.
