| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Baclofen HCl targets the GABAB receptor, a metabotropic receptor for the inhibitory neurotransmitter GABA. By binding to and activating this receptor, it mimics the action of GABA, producing slow presynaptic inhibition. This reduces the release of excitatory neurotransmitters, thereby decreasing muscle spasticity. Its therapeutic effects result from actions at both spinal and supraspinal sites.
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| ln Vitro |
Lactate dehydrogenase (LDH) activity significantly decreases in response to 1, 10 μM; 24 h HCl of baclofen, suggesting higher cell viability in striatal cells (HD19 or HD43) expressing wild-type or mutant huntingtin. ..In HD43 cells, baclofen dramatically boosts chymotrypsin-like proteasome activity and cell survival [3].
In vitro, Baclofen HCl functions as a GABAB receptor agonist. While specific IC50 values are not provided in the sources, its activity is well-characterized through its ability to inhibit neurotransmitter release in various neuronal preparations. It has also been shown to improve ubiquitin-proteasome system function and enhance cell survival in in vitro models of Huntington's disease. |
| ln Vivo |
Baclofen hydrochloride (intraperitoneal injection; 10 μg/g; twice daily for 3 days) can improve the motor deficits of YAC128 HD transgenic mice [3].
In vivo, Baclofen HCl is used clinically as an effective muscle relaxant. It is administered orally and is used to treat spasticity resulting from spinal cord injuries, multiple sclerosis, and other neurological conditions. Its efficacy in reducing muscle tone and spasms has been established through extensive clinical use. Its ability to cross the blood-brain barrier is crucial for its central effects. |
| Enzyme Assay |
A cell-free assay for Baclofen HCl would involve measuring its binding affinity to the GABAB receptor using radioligand binding techniques. In such assays, membrane preparations containing the receptor are incubated with a radiolabeled antagonist and varying concentrations of Baclofen HCl to determine its affinity. Specific protocols are not detailed in the available sources.
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| Cell Assay |
Cellular assays for Baclofen HCl typically involve electrophysiological recordings from neurons to measure its effects on synaptic transmission. The compound's ability to activate GABAB receptors and produce slow inhibitory postsynaptic potentials can be assessed in brain slice preparations or cultured neurons. These assays confirm its mechanism of action as a GABAB receptor agonist.
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| Animal Protocol |
Animal/Disease Models: 13-18 months old wild-type (WT) and mutant (MT) male YAC128 mice [3]
Doses: 10 μg/g Route of Administration: IP; twice (two times) daily at 9:00 AM and 5:00 PM , for 3 days; then a single dose was administered at 9:00 am on the fourth day. Experimental Results: Motor deficits in YAC128 HD transgenic mice were improved. Increased proteasome activity and diminished neuronal intranuclear inclusions (NII) in YAC128 HD transgenic mice. In vivo animal experiments for Baclofen HCl are not described in the available sources, as its effects are well-established through clinical use. Preclinical studies in animal models of spasticity and Huntington's disease have contributed to its development and characterization. |
| ADME/Pharmacokinetics |
Baclofen HCl is an orally active compound with high blood-brain barrier penetrance. It is well absorbed after oral administration and is metabolized in the liver. Its pharmacokinetic profile supports its use as a chronic therapy for muscle spasticity. Specific parameters such as half-life are not provided in the sources.
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| Toxicity/Toxicokinetics |
Toxicity data for Baclofen HCl are not detailed in the available sources. As a clinically used drug, its safety profile is well-established. Common adverse effects include drowsiness, dizziness, and weakness. Abrupt withdrawal can lead to severe complications. It is contraindicated in patients with certain conditions.
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| References |
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| Additional Infomation |
Baclofen HCl (CAS: 28311-31-1) is a selective GABAB receptor agonist used as a skeletal muscle relaxant. It is a lipophilic GABA derivative that crosses the blood-brain barrier. It is available as the hydrochloride salt. Its clinical use includes the treatment of spasticity from multiple sclerosis, spinal cord injuries, and other neurological disorders. It is not a research compound but an approved therapeutic agent.
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| Molecular Formula |
C10H13CL2NO2
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|---|---|
| Molecular Weight |
250.121721029282
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| Exact Mass |
249.032
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| CAS # |
28311-31-1
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| Related CAS # |
Baclofen;1134-47-0
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| PubChem CID |
6602720
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| Appearance |
White to off-white solid
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
15
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| Complexity |
191
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CC(CN)C1=CC=C(C=C1)Cl)O.Cl
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| InChi Key |
WMNUVYYLMCMHLU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H12ClNO2.ClH/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14;/h1-4,8H,5-6,12H2,(H,13,14);1H
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| Chemical Name |
4-amino-3-(4-chlorophenyl)butanoic acid;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ≥ 100 mg/mL (~399.8 mM)
DMSO: ~10 mg/mL (~40.0 mM; with ultrasonication and warming by heating to 60°C) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (10.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (10.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 1 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (10.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9981 mL | 19.9904 mL | 39.9808 mL | |
| 5 mM | 0.7996 mL | 3.9981 mL | 7.9962 mL | |
| 10 mM | 0.3998 mL | 1.9990 mL | 3.9981 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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