产品
编 号:F458472
分子式:C20H35NO2
分子量:321.5
产品类型
结构图
CAS No: 782487-28-9
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产品详情
生物活性:
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.
体内研究:
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.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.Animal Model:6-8 weeks old male CD-1 mice
Dosage:3, 10, 30 mg/kg
Administration:p.o.; daily for 3 days
Result:Significantly reduced the total number of BAL leukocytes in NSC-125066-challenged mice, up to a maximum of 60% at 7 days and 63% at 21 days at 30 mg/kg; Reduced MPO activity by 54% at Day 7 and by 74% at Day 21 at 30 mg/kg.
Animal Model:Male Sprague-Dawley rats
Dosage:10 mg/kg (Pharmacokinetic Study)
Administration:Oral administration
Result:The Cmax value is 0.830 μM and the t1/2 value is 5.2 hours.
体外研究:
Rosiptor (0.1-10 μM; 30 minutes) inhibits Akt activation in MOLT-4, but not in Jurkat cells.