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Danirixin (GSK1325756) is a potent antagonist of CXCR2 that inhibits IL-8 binding to CXCR2 (IC50: 12.5 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $56 | In Stock | |
5 mg | $113 | In Stock | |
10 mg | $189 | In Stock | |
25 mg | $353 | In Stock | |
50 mg | $562 | In Stock | |
100 mg | $793 | In Stock | |
1 mL x 10 mM (in DMSO) | $138 | In Stock |
Description | Danirixin (GSK1325756) is a potent antagonist of CXCR2 that inhibits IL-8 binding to CXCR2 (IC50: 12.5 nM). |
Targets&IC50 | CXCL8-CXCR2:12.5 nM (cell free) |
In vivo | Systemic exposure following single doses of danirixin 10 mg, 25 mg, 50 mg, 100 mg, and 200 mg increased with increasing dose. Engagement of pharmacology was demonstrated as inhibition of ex-vivo CXCL1-induced CD11b expression on peripheral blood neutrophils when compared to placebo (approximately 50 % for 50 mg and 100 mg danirixin, and 72 % at 200 mg). There was a 37 % decrease in Cmax and a 16 % decrease in AUC (0-∞) following administration of danirixin in the presence of food. Cmax also decreased by 65 % when danirixin 100 mg was administered following omeprazole 40 mg once daily for 5 days [1]. |
Alias | GSK1325756 |
Molecular Weight | 441.9 |
Formula | C19H21ClFN3O4S |
Cas No. | 954126-98-8 |
Smiles | Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(c1O)S(=O)(=O)[C@H]1CCCNC1 |
Relative Density. | 1.467 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/mL (135.78 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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