CP 465022 hydrochloride
目录号 : GC12589
AMPA receptor antagonist, non-competitive and selective
Cas No.:199655-36-2
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
CP 465022 hydrochloride is a potent and selective antagonist of AMPA receptor with IC50 value of 25 nM [1].
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA receptor) is an ionotropic transmembrane receptor for glutamate and mediates fast synaptic transmission in the central nervous system. AMPA receptors are oligomeric assemblies of four protein subunits, GluR1-4.
CP 465022 hydrochloride is a noncompetitive and selective AMPA receptor antagonist. In rat cortical neurons, CP-465022 inhibited currents induced by kainate (100 μM) with IC50 value of 25 nM and completely inhibited at concentration up to 3.2 μM. In hNT human teratocarcinoma cells, CP-465022 inhibited kainate-induced currents with IC50 value of 15 nM, which was mediated by AMPA receptors. In cultured cortical neurons stimulated by kainate, CP-465022 dose-dependently inhibited kainate-induced responses by 54% and 88% at 10 nM and 100 nM, respectively [1]. In HEK cells expressing the Nav1.6 channel, CP465022 dose-dependently inhibited Nav1.6-mediated persistent current [2].
In rats after stimulation of Schaeffer collateral/commissural pathway, CP-465022 reversibly inhibited the evoked population spike amplitude in the CA1 region. In pentylenetetrazole-induced seizure rats, CP-465022 dose-dependently reduced the incidence of tonic seizures, clonic seizures and lethality. CP-465022 inhibited vertical and horizontal locomotor activity with ED50 values of 6.6 and 11.9 mg/kg, respectively [3].
References:
[1]. Lazzaro JT, Paternain AV, Lerma J, et al. Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist. Neuropharmacology, 2002, 42(2): 143-153.
[2]. Welch NC, Lin W, Juranka PF, et al. Traditional AMPA receptor antagonists partially block Na v1.6-mediated persistent current. Neuropharmacology, 2008, 55(7): 1165-1171.
[3]. Menniti FS, Buchan AM, Chenard BL, et al. CP-465,022, a selective noncompetitive AMPA receptor antagonist, blocks AMPA receptors but is not neuroprotective in vivo. Stroke, 2003, 34(1): 171-176.
| Cas No. | 199655-36-2 | SDF | |
| 化学名 | (E)-3-(2-chlorophenyl)-2-(2-(6-((diethylamino)methyl)pyridin-2-yl)vinyl)-6-fluoroquinazolin-4(3H)-one hydrochloride | ||
| Canonical SMILES | ClC1=CC=CC=C1N(C(/C=C/C2=NC(CN(CC)CC)=CC=C2)=NC3=C4C=C(F)C=C3)C4=O.[H]Cl | ||
| 分子式 | C26H24ClFN4O.HCl | 分子量 | 499.41 |
| 溶解度 | <49.94mg/ml in DMSO | 储存条件 | Desiccate at RT |
| 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 | 2.0024 mL | 10.0118 mL | 20.0236 mL |
| 5 mM | 0.4005 mL | 2.0024 mL | 4.0047 mL |
| 10 mM | 0.2002 mL | 1.0012 mL | 2.0024 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。