| (±)-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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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。
电泳缓冲液的另一个作用是使溶液具有一定的导电性，以利于DNA分子的迁移，例如，一般电泳缓冲液中应含有0.01-0.04mol/L的Na+离子，Na+离子的浓度太低时电泳速度变慢；太高时就会造成过大的电流使胶发热甚至熔化。
电泳缓冲液还有一个组分是EDTA，加入浓度为1-2mmol/L，目的是螯合Mg2+ 等离子，防止电泳时激活 DNA酶，此外还可防止Mg2+离子与核酸生成沉淀。
