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(±)-Baclofen
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(±)-Baclofen图片
CAS NO:1134-47-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5g电议
10g电议
25g电议

产品介绍
(±)-Baclofen 是 γ-氨基丁酸 (GABA) 的亲脂性衍生物,是一种具有口服活性的选择性代谢型 GABAB 受体 (GABABR) 激动剂。
Cas No.1134-47-0
别名巴氯芬
化学名β-(aminomethyl)-4-chloro-benzenepropanoic acid
Canonical SMILESClC1=CC=C(C(CN)CC(O)=O)C=C1
分子式C10H12ClNO2
分子量213.7
溶解度≥ 3.06mg/mL in Water with gentle warming,<2.14mg/mL in DMSO
储存条件Store at 2-8°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.