GYKI 47261 dihydrochloride
目录号 : GC11259
AMPA receptor antagonist, non-competitive and selective
Cas No.:220445-20-5
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
GYKI 47261 dihydrochloride is a selective and non-competitive antagonist of AMPA receptor with IC50 value of 2.5 μM [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.
GYKI 47261 dihydrochloride is a selective and non-competitive AMPA receptor antagonist. In isolated cerebellar Purkinje cells, GYKI 47261 (10 μM) inhibited currents induced by kainate or AMPA in a non-competitive way [1]. In rat hepatocytes, GYKI-47261 (10 μM) significantly increased CYP2E1 activity. In human hepatocytes, GYKI-47261 produced the maximal induction at 0.01 μM [2].
In mice, GYKI 47261 induced muscle relaxant effects with ED50 values of 15.8-36.5 mg/kg. In a transient focal ischemia rat model, GYKI 47261 significantly reduced infarct size by 62.3-67.4%. In mice, GYKI 47261 effectively reduced oxotremorine-induced tremor and inhibited MPTP-induced neurotoxicity [1]. In Parkinson’s disease rat model, administration of GYKI-47261 and MK-801 completely normalized the response shortening induced by levodopa. In monkeys, administration of amantadine and GYKI-47261 significantly reduced dyskinesias induced by levodopa by 51% [3].
References:
[1]. Abrahám G, Sólyom S, Csuzdi E, et al. New non competitive AMPA antagonists. Bioorg Med Chem, 2000, 8(8): 2127-2143.
[2]. Tamási V, Hazai E, Porsmyr-Palmertz M, et al. GYKI-47261, a new AMPA [2-amino-3-(3-hydroxymethylisoxazole-4-yl)propionic acid] antagonist, is a CYP2E1 inducer. Drug Metab Dispos, 2003, 31(11): 1310-1314.
[3]. Bibbiani F, Oh JD, Kielaite A, et al. Combined blockade of AMPA and NMDA glutamate receptors reduces levodopa-induced motor complications in animal models of PD. Exp Neurol, 2005, 196(2): 422-429.
| Cas No. | 220445-20-5 | SDF | |
| 化学名 | 4-(8-chloro-2-methyl-11H-benzo[e]imidazo[1,2-b][1,2]diazepin-6-yl)aniline dihydrochloride | ||
| Canonical SMILES | CC1=CN2C(CC3=C(C(C4=CC=C(N)C=C4)=N2)C=C(Cl)C=C3)=N1.Cl.Cl | ||
| 分子式 | C18H15ClN4.2HCl | 分子量 | 395.71 |
| 溶解度 | <35.92mg/ml in DMSO | 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 | 2.5271 mL | 12.6355 mL | 25.271 mL |
| 5 mM | 0.5054 mL | 2.5271 mL | 5.0542 mL |
| 10 mM | 0.2527 mL | 1.2636 mL | 2.5271 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。