Baclofen [1134-47-0]
Cat# T1065-200mg
Size : 200mg
Marca : TargetMol
Baclofen
(Synonyms: Lioresal) Copy Product Info
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.
Cas No. 1134-47-0
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
COA HNMR LCMS
Product Information
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 | 213.661 |
| 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 | Pure form: -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: 2.00 mg/mL (9.36 mM), Sonication is recommended.  | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
H2O
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. | ||||||||||||||||