| 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 |
Typically exists as solid at room temperature
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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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| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (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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