CXCR2-IN-2 |
| Katalog-Nr.GC62475 |
CXCR2-IN-2 ist ein selektiver, ins Gehirn eindringender und oral bioverfÜgbarer CXCR2-Antagonist (IC50 = 5,2 nM/1 nM im β-Arrestin-Assay bzw. CXCR2-Tango-Assay).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1838123-21-9
Sample solution is provided at 25 µL, 10mM.
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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[1].
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[1].
[1]. Lu H, et al. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists. J Med Chem. 2018;61(6):2518-2532.
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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