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MedChemExpressModel Rosiptor -782487-28-9

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Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro[1][2].
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Rosiptor

MCE China:Rosiptor

Brand:MedChemExpress (MCE)

Cat. No.HY-109011

CAS:782487-28-9

Synonyms:AQX-1125

Purity:99.35%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.

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

In Vivo:Rosiptor (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 (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].

IC50 & Target:SHIP1[1] In Vitro Rosiptor (0.1-10 μM; 30 minutes) inhibits Akt activation in MOLT-4, but not in Jurkat cells[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Rosiptor Related Antibodies Western Blot Analysis[1] Cell Line: MOLT-4 cells and SHIP1-deficient Jurkat cells (IGF-1 stimulation)

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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.  [Content Brief]

[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.  [Content Brief]

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