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Baclofen GABA Receptor agonist

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

Cat.No.S4840

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 GABA Receptor agonist Chemical Structure

Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS/MSDS
Datasheet

99.79

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor TRP Channel Cholinesterase (ChE) GluR
Other GABA Receptor Inhibitors	Dihydromyricetin CGP52432 Pentylenetetrazol 4-Aminobutyric acid (GABA) (+)-Borneol Ginkgolide A Oxiracetam Emamectin Benzoate Fluralaner (-)-Borneol

Solubility

In vitro
Batch:

0.01M HCl : 3 mg/mL

Water : 0.1 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%0.01MHCL 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.15mg/ml (0.70mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified 0.01MHCL stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%0.01MHCL 1 95 %Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.021mg/ml (0.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 0.42 mg/ml clear 0.01MHCL stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	213.66	Formula	C₁₀H₁₂ClNO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1134-47-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			SMILES	C1=CC(=CC=C1C(CC(=O)O)CN)Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	GABAB receptor
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.
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. This compound might suppress cytodestructive autophagic activity through Akt-GSK-3β-p-mTOR-Beclin 1 signaling pathway under chronic cerebral hypoperfusion. During brain ischemia, it could reduce CX43 and CX36 surface expression. Baclofen-induced suppression of increased CX43 and CX36 surface expressions helps neurons survive. This chemical reduces reinstatement to cocaine self-administration in an animal model of relapse. It suppresses Bel-7402 xenograft tumor growth in vivo.
References	[1] https://www.nature.com/articles/srep14474#discussion [2] https://pubmed.ncbi.nlm.nih.gov/12629530/ [3] https://pubmed.ncbi.nlm.nih.gov/18222491/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-05-13)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07560878	RECRUITING	Major Depression	Mclean Hospital	2026-03-11	EARLY_PHASE1
NCT06835907	RECRUITING	Alcohol Use Disorder (AUD)	Universitair Ziekenhuis Brussel	2024-10-28
NCT06606574	RECRUITING	Dystonic Cerebral Palsy	Baylor College of Medicine	2024-11-01
NCT06564714	NOT_YET_RECRUITING	Traumatic Spinal Cord Injury	Centre Integre Universitaire de Sante et Services Sociaux du Nord de l'ile de Montreal	2024-12	PHASE4
NCT05935553	RECRUITING	Benzodiazepine Dependence	Hospices Civils de Lyon	2026-01-15	PHASE2; PHASE3
NCT07378046	RECRUITING	Herpes Zoster; Pain	Beijing Tiantan Hospital	2025-12-15

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