Hazard Information | Back Directory | [Description]
AZD8309 is an oral CXCR2 antagonist. | [Uses]
AZD8309 is an orally active antagonist of CXCR2. AZD8309 has the ability to regulate the transmigration of neutrophils. AZD8309 can be used in the study of inflammatory diseases[1]. | [in vivo]
AZD8309 (50 mg/kg; p.o.; twice daily) reduces neutrophil migration and pancreatic protease activation in experimental pancreatitis in mice[1]. Animal Model: | Male C57BL6 mice (25-30 g) with experimental pancreatitis[1] | Dosage: | 50 mg/kg | Administration: | Oral gavage; twice daily starting 3 h prior to pancreatitis induction | Result: | Significantly reduced MPO in the pancreas and lungs (8 h & 24 h) and reduced intrapancreatic trypsin and elastase activity (8 h) in caerulein-pancreatitis.
Reduced serum cytokine levels as well as histopathological damage. |
| [IC 50]
CXCR2: 4 nM (IC50) | [References]
[1] Malla SR, et al. Effect of oral administration of AZD8309, a CXCR2 antagonist, on the severity of experimental pancreatitis. Pancreatology. 2016 Sep-Oct;16(5):761-9. DOI:10.1016/j.pan.2016.07.005 [2] Walters I, Austin C, Austin R, et al. Evaluation of a series of bicyclic CXCR2 antagonists. Bioorg Med Chem Lett. 2008;18(2):798-803. DOI:10.1016/j.bmcl.2007.11.039 |
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