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编 号:F709430
分子式:C18H23ClN2O5S
分子量:414.9
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.

体内研究:
CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models.Animal Model:6-8 week old male C57Bl/6 mice (Air Pouch Model in Mouse)
Dosage:1, 3, and 10 mg/kg
Administration:P.o.; twice daily for 3 days
Result:Significantly inhibited neutrophil infiltration into mouse air pouch.
Animal Model:8-10 week old male Wistar rats (Air Pouch Model in Rat)
Dosage:1, 3, and 10 mg/kg
Administration:P.o.; twice daily for 3 days
Result:Inhibited neutrophil migration to air pouch in rat.
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