Lu AF27139
目录号 : GC63996
Lu AF27139 是一种有效的、选择性的、具有口服活性的 P2X7 受体拮抗剂（IC50s 值对人和大鼠分别为 12 和 2.4 nM，Kis 对小鼠、人和大鼠分别为 22、54 和 13 nM ）。Lu AF27139 具有啮齿动物活性和 CNS 渗透特性。Lu AF27139 具有研究中枢神经系统疾病的潜力。
Cas No.:2097117-06-9
Sample solution is provided at 25 µL, 10mM.
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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[1].
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[1].Lu AF27139 (compound 1) (100 nM) inhibits 300 μM BzATPinduced current in primary rat microglia with 80% inhibition occurring at a 100 nM dose[1].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[1].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[1].
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[1].Assessment of Pharmacokinetics (PK) profile of Lu AF27139 (compound 1) in rat[1]. dose Cu, plasma (nM)a Cu, brain (nM)aCu, spinal cord (nM)a (mg/kg, po) (1 h) (2 h) (1 h)(2 h)(1 h)(2 h) T1 22.4 ± 4.2 22.8 ± 10 5.4 ± 2.6 6.4 ± 2.05.20 ± 0.8010.0 ± 2.0a: 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.
[1]. Hopper AT, et al. Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. J Med Chem. 2021;64(8):4891-4902.
| Cas No. | 2097117-06-9 | SDF | Download SDF |
| 分子式 | C21H19ClF3N5O2S | 分子量 | 497.92 |
| 溶解度 | DMSO : 125 mg/mL (251.04 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0084 mL | 10.0418 mL | 20.0835 mL |
| 5 mM | 0.4017 mL | 2.0084 mL | 4.0167 mL |
| 10 mM | 0.2008 mL | 1.0042 mL | 2.0084 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet