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(±)-Baclofen

Catalog No.GC12927

El (±)-baclofeno, un derivado lipófilo del ácido γ-aminobutírico (GABA), es un agonista metabotrópico selectivo del receptor GABAB (GABABR) activo por vía oral.

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(±)-Baclofen Chemical Structure

Cas No.: 1134-47-0

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
34,00 $
Disponible
5g
73,00 $
Disponible
10g
131,00 $
Disponible
25g
239,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 1134-47-0 SDF
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 Water with gentle warming, <2.14mg/mL in DMSO Storage Store at 2-8°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 4.6795 mL 23.3973 mL 46.7946 mL
5 mM 0.9359 mL 4.6795 mL 9.3589 mL
10 mM 0.4679 mL 2.3397 mL 4.6795 mL
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Review for (±)-Baclofen

Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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