Product IntroductionBioactivity英文名:
Rosiptor描述: Rosiptor (AQX-1125) 是一种选择性,具有口服活性的磷酸酶 SHIP1激活剂。它在体外抑制 Akt 磷酸化、炎症介质生成和白细胞趋化,具有抗炎作用。
细胞实验: Cell Line: MOLT-4 cells and SHIP1-deficient Jurkat cells (IGF-1 stimulation) [1]. Concentration: 0.1, 1, 10 μM. Incubation Time: 30 minutes
动物实验: Animal Model: 6-8 weeks old male CD-1 mice[1]. Dosage: 3, 10, 30 mg/kg. Administration: p.o., daily for 3 days
体外活性: In MOLT-4 but not Jurkat cells, Rosiptor (0.1-10 μM, 30 minutes) inhibits Akt activation [1].
体内活性: 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]. 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].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 145 mg/mL (451 mM)
关键字:
AQX1125 |
Phosphatase |
Rosiptor |
Inhibitor |
AQX 1125 |
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