计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor ( IC 50 s of 12 and 2.4 nM for human and rat, K i s 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
In Vitro
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 IC 50 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 IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . dose C u, plasma (nM) a C u, brain (nM) a C u, spinal cord (nM) a (mg/kg, po) (1 h) (2 h) (1 h) (2 h) (1 h) (2 h) T 1 22.4 ± 4.2 22.8 ± 10 5.4 ± 2.6 6.4 ± 2.0 5.20 ± 0.80 10.0 ± 2.0 a: Free plasma, brain, and spinal cord concentrations of Lu AF27139 in rat were determined by the formula (Ct*f u ), where Ct is the total tissue (plasma, brain, or spinal cord) drug concentration and f u is the fraction unbound in these tissues as determined by ex vivo equilibrium dialysis. Values are expressed as mean ± SEM for n = 3 animals. f u , plasma = 0.02 ± 0.00, f u , spinal cord = 0.07 ± 0.03, and f u , brain = 0.09 ± 0.03. Values are expressed as mean ± SEM for n ≥ 3 experiments. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
IC50& Target:P2X7
规格
规格或纯度
10mM in DMSO
英文名称
Lu AF27139
生化机理
Lu AF27139 是一种强效、选择性和口服活性的 P2X7 受体拮抗剂（人和大鼠的 IC 50 s 分别为 12 和 2.4 nM，小鼠、人和大鼠的 K i s 分别为 22、54 和 13 nM）。Lu AF27139 具有鼠药活性和中枢神经系统穿透性。L
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
名称和识别符
分子类型
小分子
分子量
497.92
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2097117-06-9，分子式为 C21H19ClF3N5O2S，分子量为 497.92 g/mol。
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