| Identification | Back Directory | [Name]
CXCR2-IN-68 | [CAS]
1838123-21-9 | [Synonyms]
CXCR2-IN-2
CXCR2-IN-68
Urea, N-[4-chloro-2-hydroxy-3-[[(3S)-tetrahydro-3-methyl-3-furanyl]sulfonyl]phenyl]-N'-[(1R)-2-methyl-2-cyclopenten-1-yl]- | [Molecular Formula]
C18H23ClN2O5S | [MDL Number]
MFCD33548813 | [MOL File]
1838123-21-9.mol | [Molecular Weight]
414.9 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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]. | [in vivo]
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]. | Animal Model: | 6-8 week old male C57Bl/6 mice (Air Pouch Model in Mouse)[1] | | Dosage: | 1, 3, and 10 mg/kg | | Administration: | P.o.; twice daily for 3 days | | Result: | Significantly inhibited neutrophil infiltration into mouse air pouch.
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| Animal Model: | 8-10 week old male Wistar rats (Air Pouch Model in Rat)[1] | | 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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| [IC 50]
CXCR2: 5.2 nM (IC50); CXCR1: 3.8 μM (IC50) | [storage]
Store at -20°C | [References]
[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. |
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