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Biochem/physiol Actions
Danirixin (GSK1325756) is an orally active, selective CXC chemokine receptor 2 (CXCR2) antagonist with 78-fold lower affinity toward CXCR1 (CXCR2/CXCR1 IC50 = 12.5/977 nM by competitive binding against 0.225 nM [125I] CXCL8). Danirixin blocks agonist-induced neutrophil CD11b expression in vitro (IC50 = 420/890 nM against induction by 10 nM human CXCL1/rat CXCL2 using rat/human whole blood) and prevents lung neutrophils influx in rats in vivo following aerosol lipopolysaccharide or ozone challenge (ED50 = 1.4 and 16 mg/kg, respectively).
Orally active, selective CXC chemokine receptor 2 (CXCR2) antagonist.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (Warmed) |
| storage temp. | -10 to -25°C |
| SMILES string | O=C(NC1=CC=C(C(S([C@H]2CCCNC2)(=O)=O)=C1O)Cl)NC3=C(C(F)=CC=C3)C |
| InChI key | NGYNBSHYFOFVLS-LBPRGKRZSA-N |
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¥ 12156.68
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¥ 1148.92
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¥ 4164.19
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¥ 2013.69
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¥ 3442.25
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¥ 1476.00
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