| (±)-BaclofenGABAB agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.35%
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| Cas No. | 1134-47-0 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | β-(aminomethyl)-4-chloro-benzenepropanoic acid | ||
| Canonical SMILES | ClC1=CC=C(C(CN)CC(O)=O)C=C1 | ||
| Formula | C10H12ClNO2 | M.Wt | 213.7 |
| Solubility | ≥3.06mg/mL in H2O with gentle warming, <2.14mg l="" in="" dmso=""> | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 200 nM: a selective agonist of γ-Aminobutyric acid metabotropic receptor (B) (GABAB).
(±)-Baclofen, a selective agonist of GABAB, causes skeletal muscle relaxation and inhibits spasticity via triggering GABAB. (±)-Baclofen, as an active anti-craving medication, modifies animal responses to alcohol and cocaine. γ-Aminobutyric acid (GABA), an inhibitory neurotransmitter, acts via heteromeric ligand-gated ion channels, GABAA and GABAC, and a G protein-coupled receptor, GABAB.
In vitro: (±)-Baclofen dampened cell growth in human hepatocellular carcinoma (HCC) cells in a dose-dependent manner. (±)-Baclofen also caused cell cycle arrest at G0/G1 phase without inducing cell death. Additionally, (±)-baclofen-evoked HCC cells proliferation was associated with down-regulation of the intracellular cAMP level, up-regulation of p21WAF1 protein expression and its phosphorylation level, which could be reversed by pretreatment with the GABAB antagonist, phaclofen, indicating that (±)-baclofen-evoked growth blockade was exerted in a GABAB-dependent fashion [1].
In vivo: The mice, subcutaneously injected with Bel-7402 cells, were given an intraperitoneal injection of (±)-baclofen 30 mg/kg every day for 30 days. Compared with the control, (±)-baclofen remarkably blocked the Bel-7402 xenograft tumor growth without causing toxic effects via measuring the relative tumor volume and the mean body weight change in (±)-baclofen-treated groups, which could make (±)-baclofen as an effective and relatively safe potential drug for the treatment of HCC [1].
Reference:[1]. Wang, T., Huang, W., & Chen, F. Baclofen, a GABAB receptor agonist, inhibits human hepatocellular carcinoma cell growth in vitro and in vivo. Life Sciences. 2008; 82(9-10): 536-541.
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最好是测浓度，一般不超过30-40ug，上样缓冲液一般4×或者5×，这个没太大区别。
1。称量氨基丁三醇 242g，Na2EDTA.2H2O 37.2g 于1L烧杯中；
2。向烧杯中加入约600ml去离子水，充分搅拌均匀；
3。加入57.1ml的冰乙酸，充分溶解；
4。用NaOH调pH至8.3，加去离子水定容至1L后，室温保存。
使用时稀释50倍 即1×TAE Buffer
10×TBE Buffer配制方法：
1。称量氨基丁三醇 108g，Na2EDTA.2H2O 7.44g，硼酸55g 于1L烧杯中；
2。加入约700ml去离子水，搅拌均匀；
3。用NaOH调pH至8.3，加去离子水定容至1L后，室温保存。
使用时稀释10倍 即1×TBE Buffer
2乘SDS-PAGE上样缓冲液（20ml体系）
1.0mol/L Tris-HCL (pH 6.8) 2ml
1.0mol/L DTT 4ml
SDS 0.8g
溴芬蓝 0.04g
甘油 4ml
dd水 定容至20ml
4℃冰箱保存，可以不分装，我们实验室一般用三个月以上
先配1.0mol/L的DTT,双蒸无菌水溶解4℃冰箱保存,配上样缓冲液的时候加入就可以了,都混匀保存也没问题的
配制分三步： 1) 1 M Tris-HCl (pH 8.0) 50 ml的配制：称取Tris碱6.06 g，加超纯水40 ml溶解，滴加浓HCl约2.1 ml调pH至8.0，定容至50 ml。
① 上样缓冲液中包括甘油,溴酚蓝,SDS等,甘油主要作用是防止样品漂浮出点样孔,溴酚蓝作为电泳指示剂,用来观察电泳进度,SDS用于一些核酸结合蛋白的变性解离.
②核酸染料与凝胶中核酸结合,以便于在紫外光下显示核酸条带.
