产品
编 号：F741551
分子式：C21H24F3N5O2
分子量：435.44
分子式：C21H24F3N5O2
分子量：435.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 2410393-15-4
产品详情
生物活性：
HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.
体内研究：
HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis.HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL.HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human.HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively.Animal Model:A rat model of collagen induced arthritis (CIA).
Dosage:15, 50, 150 mg/kg.
Administration:PO, once daily.
Result:Led to a significant reduction in paw swelling as compared to vehicle control, with a minimum effective dose at 15 mg/kg QD. Notably, at 150 mg/kg QD, HS271 eliminated the paw swelling.
HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.
体内研究：
HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis.HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL.HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human.HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively.Animal Model:A rat model of collagen induced arthritis (CIA).
Dosage:15, 50, 150 mg/kg.
Administration:PO, once daily.
Result:Led to a significant reduction in paw swelling as compared to vehicle control, with a minimum effective dose at 15 mg/kg QD. Notably, at 150 mg/kg QD, HS271 eliminated the paw swelling.
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