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AQX 1125 acetate

Names

[ CAS No. ]:
782487-29-0

[ Name ]:
AQX 1125 acetate

[Synonym ]:
AQX-1125
AQX 1125
AQX1125
(1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexan-1-ol

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase

[Target]

SHIP1[1]


[In Vitro]

Rosiptor acetate (0.1-10 μM; 30 minutes) inhibits Akt activation in MOLT-4, but not in Jurkat cells[1].

[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.  

[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C22H39NO4

[ Molecular Weight ]:
381.55

[ Exact Mass ]:
321.26700

[ PSA ]:
66.48000

[ LogP ]:
3.80370

Related Compounds