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Baclofen

Name: Baclofen
Brand: Selleck Chemicals
SKU: S4840
Rating: 5 (1 reviews)

Catalog No.S4840 Purity: 99.79%

Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.

Baclofen Chemical Structure

CAS: 1134-47-0

Purity & Quality Control

Batch: S484001 0.01M HCl] 3 mg/mL] true] Water] 0.1 mg/mL] false] DMSO] Insoluble] false Purity: 99.79%

99.79

Baclofen Related Products

Related Targets	GABAA receptor GABAB receptor	Click to Expand
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Signaling Pathway

GABA Receptor Signaling Pathway

Choose Selective GABA Receptor Inhibitors

Biological Activity

Description

Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.

Targets

GABAB receptor ^[2]

In vitro
In vitro	Baclofen induces G0/G1 phase arrest which is connected with down-regulation of intracellular cAMP level, and up-regulation of p21^WAF1 protein expression as well as its phosphorylation level in human hepatocellular carcinoma cell^[3].
Cell Research	Cell lines	Bel-7402, HuH-7, and HepG2 cells
	Concentrations	25, 50 and 100 μM
	Incubation Time	0-4 days
	Method	Bel-7402, HuH-7, and HepG2 cells are seeded into 96-well plates (10,000 per well) in a final volume of 200 μl medium. After a 24-hour attachment, cells are incubated with Bac (25, 50 and 100 μM) in the absence or presence of Pha (100 μM) for indicated time intervals. During this time, the culture medium is replaced with fresh medium every 24 h. After treatment, cell proliferation is evaluated by MTS assay. The OD values are measured at 490 nm with a microplate spectrophotometer.

In Vivo
In vivo	Chronic treatment with baclofen markedly diminishes hippocampal atrophy and neuronal apoptosis in hippocampal CA1 area via the regulation of autophagy in chronic cerebral hypoperfusion in rats. Baclofen might suppress cytodestructive autophagic activity through Akt-GSK-3β-p-mTOR-Beclin 1 signaling pathway under chronic cerebral hypoperfusion. During brain ischemia, baclofen could reduce CX43 and CX36 surface expression. Baclofen-induced suppression of increased CX43 and CX36 surface expressions helps neurons survive^[1]. Baclofen reduces reinstatement to cocaine self-administration in an animal model of relapse^[2]. Baclofen suppresses Bel-7402 xenograft tumor growth in vivo^[3].
Animal Research	Animal Models	male Sprague-Dawley rats of clean grade, aged 2-3 months, weighing 220-250 g
	Dosages	12.5 mg/kg and 25 mg/kg
	Administration	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06175507	Not yet recruiting	Alcohol Liver Disease	Institute of Liver and Biliary Sciences India	December 25 2023	Not Applicable
NCT04603625	Recruiting	Quadriplegic Cerebral Palsy	Azienda Unità Sanitaria Locale Reggio Emilia\|Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta\|Ospedale IRCCS G. Gaslini di Genova\|IRCCS Eugenio Medea\|IRCCS Don Carlo Gnocchi di Firenze\|Azienda Unita'' Sanitaria Locale Di Modena\|Azienda Usl di Bologna\|Azienda Unità Sanitaria Locale della Romagna\|Azienda ULSS di Verona e Provincia\|Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico	October 29 2020	Not Applicable
NCT04509336	Terminated	Cirrhosis	Mansoura University	August 20 2020	Not Applicable
NCT04471714	Withdrawn	Spasticity Muscle\|Spinal Cord Injuries	University of Alberta	January 10 2020	Phase 2
NCT03682978	Completed	Autism Spectrum Disorder	Celso Arango MD PhD\|UMC Utrecht	September 19 2019	Phase 2

References

Chemical Information & Solubility

Molecular Weight	213.66	Formula	C₁₀H₁₂ClNO₂
CAS No.	1134-47-0	SDF	--
Smiles	C1=CC(=CC=C1C(CC(=O)O)CN)Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

0.01M HCl : 3 mg/mL

Water : 0.1 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

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In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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