CGP 13501
目录号 : GC13374
Positive modulator of GABAB receptors,allosteric
Cas No.:56189-68-5
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
CGP 13501 is a positive allosteric modulator of GABAB receptor [1].
The GABAB receptor is a metabotropic transmembrane receptors for GABA that is linked via G-protein to potassium channel. It stimulates the opening of K+ channel and hyperpolarize the neuron.
CGP 13501 is a positive allosteric modulator of GABAB receptor. In Chinese hamster ovary (CHO) cell line expressing GABAB(1b/2), CGP 13501 potentiated GABA-stimulated GTPγ[35S] binding to cell membranes [1]. In rat cortex, CGP13501 (10 μM) enhanced GABA-mediated activation of Gαo and increased GTPγ[35S] binding in the presence of GABA. Also, in the hippocampus and cerebellum, CGP13501 increased GABA-induced GTPγ[35S] binding and activation of Gαo. In rat cortex, hippocampus and cerebellum, CGP55845A blocked the influence of CGP13501 on GABA-induced GTPγ[35S] binding at Gαo with pIC50 values of 7.4, 7.31 and 6.82, respectively. In cells expressing GABAB(1b+2) receptors, CGP13501 increased GTPγ[35S] binding at Gαi1/3 [2].
References:
[1]. Urwyler S, Mosbacher J, Lingenhoehl K, et al. Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol Pharmacol, 2001, 60(5): 963-971.
[2]. Rasheed N, Ahmad A, Al-Sheeha M, et al. Neuroprotective and anti-stress effect of A68930 in acute and chronic unpredictable stress model in rats. Neurosci Lett, 2011, 504(2): 151-155.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4431 mL | 17.2153 mL | 34.4305 mL |
| 5 mM | 0.6886 mL | 3.4431 mL | 6.8861 mL |
| 10 mM | 0.3443 mL | 1.7215 mL | 3.4431 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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