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Rosiptor (AQX-1125) acetate is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor acetate (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro[1][2]. | [in vivo]
Rosiptor acetate (3-30 mg/kg; p.o.; daily for 3 days) significantly reduces the total number of BAL leukocytes in NSC-125066-challenged mice and reduces MPO activity[2].
Rosiptor acetate (10 mg/kg; p.o.) has the Cmax value of 0.830 μM and the t1/2 value of 5.2 hours. AQX-1125 also exhibits >80% oral bioavailability[1]. | [References]
[1] Stenton GR, et al. Characterization of AQX-1125, a small-molecule SHIP1 activator: Part 1. Effects on inflammatory cell activation and chemotaxis in vitro and pharmacokinetic characterization in vivo. Br J Pharmacol. 2013 Mar;168(6):1506-18. DOI:10.1111/bph.12039
[2] Cross J, et al. AQX-1125, small molecule SHIP1 activator inhibits NSC-125066-induced pulmonary fibrosis. Br J Pharmacol. 2017 Sep;174(18):3045-3057. DOI:10.1111/bph.13934 |
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