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Baclofen (Alias: Lioresal)

Catalog No. T1065 Copy Product Info
Purity: 99.94%
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Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

Baclofen

Copy Product Info
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Catalog No. T1065
Alias Lioresal

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

Baclofen
Cas No. 1134-47-0
Pack SizePriceUSA StockGlobal StockQuantity
200 mg$31In StockIn Stock
500 mg$46In StockIn Stock
1 g$61In StockIn Stock
5 g$237-In Stock
In stock · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.94%
Color:White
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Product Introduction

Baclofen AI Summary
Baclofen demonstrates significant anticonvulsant activity and interacts with Gamma-aminobutyric acid (GABA) receptors. It shows efficacy in the maximal electroshock seizure test and the subcutaneous pentylenetetrazole seizure threshold test at 50.0 mg/kg, along with a TD50 of 47.0 mg/kg in the rotarod toxicity test in mice. The compound displays high selectivity for the GABA-B receptor, with potent inhibition of [3H]-baclofen binding (IC50 = 35.0 nM) and exhibits much weaker inhibition on the GABA-A receptor (IC50 = 1047000.0 nM). Additionally, Baclofen shows various effects such as anxiolytic properties, muscle relaxant, and analgesic effects in mice, modulating CaV2.2 channels, and influencing multiple blood and liver parameters. It also shows limited brain penetration in rats but better distribution in human CSF. Baclofen has shown antiviral activity against SARS-CoV-2, inhibiting the virus-induced cytotoxicity in cell assays. Despite inducing some liver toxicity in humans, it appears to have a low risk of causing chronic liver diseases. Its pharmacokinetic profile includes a maximum concentration (Cmax) of 748.85 nM and a bioavailability (F) of 70.0%. The compound has no significant inhibition of major human transporters like BSEP, MRP2, and others..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.
SynonymsLioresal
Chemical Properties
Molecular Weight213.66
FormulaC10H12ClNO2
Cas No.1134-47-0
SmilesNCC(CC(O)=O)C1=CC=C(Cl)C=C1
Relative Density.1.285 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: Insoluble
H2O: 2.5 mM, Sonication is recommended.
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM4.6803 mL23.4017 mL46.8033 mL234.0167 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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