产品
编 号：F741368
分子式：C21H19ClF3N5O2S
分子量：497.92
分子式：C21H19ClF3N5O2S
分子量：497.92
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2097117-06-9
产品详情
生物活性：
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
体内研究：
Lu AF27139 (compound 1) (p.o.; 3, 10, and 100 mg/kg) reduces intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.Assessment of Pharmacokinetics (PK) profile of Lu AF27139 (compound 1) in rat. doseCu, plasma (nM)aCu, brain (nM)aCu, spinal cord (nM)a
(mg/kg, po)(1 h)(2 h)(1 h)(2 h)(1 h)(2 h)
T122.4 ± 4.222.8 ± 105.4 ± 2.66.4 ± 2.05.20 ± 0.8010.0 ± 2.0
a: Free plasma, brain, and spinal cord concentrations of Lu AF27139 in rat were determined by the formula (Ct*fu), where Ct is the total tissue (plasma, brain, or spinal cord) drug concentration and fu is the fraction unbound in these tissues as determined by ex vivo equilibrium dialysis. Values are expressed as mean ± SEM for n = 3 animals. fu, plasma = 0.02 ± 0.00, fu, spinal cord = 0.07 ± 0.03, and fu, brain = 0.09 ± 0.03. Values are expressed as mean ± SEM for n ≥ 3 experiments.Animal Model:Male Sprague?Dawley rats (280?350 g); Male C57BL mice (18?25g)
Dosage:3, 10, and 100 mg/kg
Administration:p.o.
Result:Reduced intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.
体外研究：
Lu AF27139 (compound 1) (10-200 nM) inhibits 100 μM BzATP-induced current in HEK293 cells stably transfected with the rat P2X7R in a dose response manner with an IC50 of 66 nM.Lu AF27139 (compound 1) (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose.Lu AF27139 (compound 1) inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC50 of 38 ± 2.5 nM.Lu AF27139 (compound 1) concentration-dependently blocks IL-1β release in rat and mouse primary cortical microglia primed with LPS and induces with 1 mM BzATP with IC50’s of 38 ± 19 nM in rat and 26 ± 6 nM in mice.
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases.
体内研究：
Lu AF27139 (compound 1) (p.o.; 3, 10, and 100 mg/kg) reduces intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.Assessment of Pharmacokinetics (PK) profile of Lu AF27139 (compound 1) in rat. doseCu, plasma (nM)aCu, brain (nM)aCu, spinal cord (nM)a
(mg/kg, po)(1 h)(2 h)(1 h)(2 h)(1 h)(2 h)
T122.4 ± 4.222.8 ± 105.4 ± 2.66.4 ± 2.05.20 ± 0.8010.0 ± 2.0
a: Free plasma, brain, and spinal cord concentrations of Lu AF27139 in rat were determined by the formula (Ct*fu), where Ct is the total tissue (plasma, brain, or spinal cord) drug concentration and fu is the fraction unbound in these tissues as determined by ex vivo equilibrium dialysis. Values are expressed as mean ± SEM for n = 3 animals. fu, plasma = 0.02 ± 0.00, fu, spinal cord = 0.07 ± 0.03, and fu, brain = 0.09 ± 0.03. Values are expressed as mean ± SEM for n ≥ 3 experiments.Animal Model:Male Sprague?Dawley rats (280?350 g); Male C57BL mice (18?25g)
Dosage:3, 10, and 100 mg/kg
Administration:p.o.
Result:Reduced intracerebroventricular (icv) administered LPS-primed and BzATP-triggered IL-1β release in the frontal cortex of rats and mice.
体外研究：
Lu AF27139 (compound 1) (10-200 nM) inhibits 100 μM BzATP-induced current in HEK293 cells stably transfected with the rat P2X7R in a dose response manner with an IC50 of 66 nM.Lu AF27139 (compound 1) (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose.Lu AF27139 (compound 1) inhibits LPS-primed and BzATP-induced IL-1β release from THP-1 cells with an IC50 of 38 ± 2.5 nM.Lu AF27139 (compound 1) concentration-dependently blocks IL-1β release in rat and mouse primary cortical microglia primed with LPS and induces with 1 mM BzATP with IC50’s of 38 ± 19 nM in rat and 26 ± 6 nM in mice.
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