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Baclofen
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Catalog No. T1065Cas No. 1134-47-0
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
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Purity: 99.66%
Catalog No. T1065Alias LioresalCas No. 1134-47-0
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.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 200 mg | $31 | In Stock | In Stock | |
| 500 mg | $46 | In Stock | In Stock | |
| 1 g | $61 | In Stock | In Stock | |
| 5 g | $237 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.66%
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
Chemical Properties
Storage & Solubility Information
| 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. |
| Synonyms | Lioresal |
| Molecular Weight | 213.66 |
| Formula | C10H12ClNO2 |
| Cas No. | 1134-47-0 |
| Smiles | NCC(CC(O)=O)C1=CC=C(Cl)C=C1 |
| Relative Density. | 1.285 g/cm3 |
| Storage | Powder: -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
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Calculator
In Vivo Formulation Calculator (Clear solution)
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:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
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 DMSO 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 DMSO stock solution to 400 μL PEG300 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 ddH2O 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.
Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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