CP-465022 (maleate)
目录号 : GC12742
An AMPA receptor antagonist
Cas No.:199656-46-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 25 nM for AMPA receptor-mediated currents in rat cortical neurons
CP-465022 is an AMPA antagonist.
The inhibition of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor has been hypothesized to lead to neuroprotective efficacy after cerebral ischemia on the basis of the activity in ischemia models of a variety of compounds with varying selectivity for AMPA over other glutamate receptor subtypes.
In vitro: CP-465022 inhibited AMPA receptor-mediated currents in rat cortical neurons and such inhibition was found to be noncompetitive with agonist concentration. CP-465022 was selective for AMPA over kainate and N-methyl-D-aspartate receptors. However, CP-465022 was found to be equipotent for AMPA receptors composed of different AMPA receptor subunit combinations, which indicated that CP-465022 is equivalently potent for inhibition of AMPA receptor-mediated responses in different types of neurons expressing different AMPA receptor subunits [1].
In vivo: Animal study showed that CP-465022 could potently and efficaciously inhibit AMPA receptor-mediated hippocampal synaptic transmission and the induction of seizures. However, at comparable doses, CP-465022 failed to prevent CA1 neuron loss after brief global ischemia or to reduce infarct volume after temporary middle cerebral artery occlusion [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Lazzaro JT, Paternain AV, Lerma J, Chenard BL, Ewing FE, Huang J, Welch WM, Ganong AH, Menniti FS. Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist. Neuropharmacology. 2002 Feb;42(2):143-53.
[2] Menniti FS, Buchan AM, Chenard BL, Critchett DJ, Ganong AH, Guanowsky V, Seymour PA, Welch WM. CP-465,022, a selective noncompetitive AMPA receptor antagonist, blocks AMPA receptors but is not neuroprotective in vivo. Stroke. 2003 Jan;34(1):171-6.
| Cas No. | 199656-46-7 | SDF | |
| 化学名 | 3-(2-chlorophenyl)-2-[2-[6-[(diethylamino)methyl]-2-pyridinyl]ethenyl]-6-fluoro-4(3H)-quinazolinone-(2Z)-2-butenedioate | ||
| Canonical SMILES | FC1=CC=C2C(C(N(C3=C(Cl)C=CC=C3)C(/C=C/C4=CC=CC(CN(CC)CC)=N4)=N2)=O)=C1.OC(/C=C\C(O)=O)=O | ||
| 分子式 | C26H24ClFN4O • C4H4O4 | 分子量 | 579.0 |
| 溶解度 | Soluble in DMSO | 储存条件 | Room temperature |
| 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 | 1.7271 mL | 8.6356 mL | 17.2712 mL |
| 5 mM | 0.3454 mL | 1.7271 mL | 3.4542 mL |
| 10 mM | 0.1727 mL | 0.8636 mL | 1.7271 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。
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