产品
编 号:F197648
分子式:C22H17ClFN9O
分子量:477.88
产品类型
结构图
CAS No: 1640247-87-5
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产品详情
生物活性:
GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis.
体内研究:
GS-9901 (0.3/1/3 mg/kg, orally,twice daily for 7 days) demonstrates efficacy in a rat model of arthritis and is predicted to be suitable for q.d. dosing in humans.Animal Model:Female Lewis rats with established collagen-induced arthritis (CIA).
Dosage:0.3 mg/kg, 1 mg/kg, and 3 mg/kg.
Administration:Orally, twice-daily for 7 days starting on the 10th day after the second collagen immunization.
Result:Demonstrated significant reduction in ankle swelling in rats treated with 0.3 mg/kg 35 (31% reduction), 1 mg/kg 35 (67%), and 3 mg/kg 35 (65%). Plasma concentrations measured on day 7 (12 h after last dose) were consistent with maintaining approximately 60%, 80%, and >90% inhibition of PI3Kδ at 0.3, 1.0, and 3 mg/kg doses, respectively, at trough levels.