ROSiptor 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。
产品描述
Rosiptor (AQX-1125) is an orally-active and specific phosphatase SHIP1 activator with anti-inflammatory effects.
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].
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
Cas No.
782487-28-9
分子式
C20H35NO2
分子量
321.5
别名
AQX-1125;洛司普托
储存和溶解度
DMSO:145 mg/mL (451 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years