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| 500mg |
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Purity: ≥98%
Baclofen (also known as STX 209) is a derivative of gamma-aminobutyric acid and a selective GABAB receptor agonist.primarily used to treat spasticity. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing It acts at spinal and supraspinal sites, reducing excitatory transmission. GABAB receptors are metabotropic receptors which produce slow inhibitory signals.
| Targets |
GABABR/GABAB receptor
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|---|---|
| ln Vitro |
Lactate dehydrogenase (LDH) activity was significantly reduced in striatal cells (HD19 or HD43) expressing wild-type or heterogeneous huntingtin after being exposed to 1, 10 μM of baclofen for 24 hours. This suggests that the cells were more viable. In HD43 cells, baclofen dramatically boosts both cell survival and chymotrypsin-like pancreatic body activity [3].
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| ln Vivo |
In YAC128 HD buttons, baclofen (i.p. ; 10 μg/g; twice daily for three days) improves motor deficits [3].
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| Enzyme Assay |
Proteasome activity determination [3]
Proteasome activity was determined by measuring the fluorescence of 7-amido-4-methylcoumarin (AMC; excitation 380 nm, emission 460 nm) generated from peptide-AMC linked substrates. Reactions were conducted in a final volume of 200 μl of buffer including 50 mM Tris–HCl (pH 7.5) and 1 mM EDTA. After adding samples to the reaction mixtures, reactions were initiated by adding the substrate Suc-Leu-Leu-Val-Try-AMC (65 μM) to measure chymotrypsin-like activity. Reactions progressed for 360 min at 25 °C. Enzymatic activity was expressed as fluorescence units (FU)/mg/min of protein. |
| Cell Assay |
Cell culture and in vitro baclofen treatment [3]
Tet-off inducible wild type (HD19, 26 CAG repeats) and mutant (HD43, 105 CAG repeats) striatal cells were cultured at 33 °C in Dulbecco’s Modified Eagle’s Medium (DMEM; Hyclone, Logan, UT) supplemented with 10% fetal bovine serum (Hyclone), 2 mM l-glutamine (Sigma, St. Louis, MO), penicillin, and streptomycin. Expression of the huntingtin gene was induced by administration of doxycycline (1 μg/ml) for 24 h. The selective GABAB receptor agonist, baclofen (RS-baclofen; Tocris Cookson, Ellisville, MO), was administered to cultured cells at the indicated concentrations. After 24 h of administration, cell culture medium was collected for cell viability assays. Cells were harvested and lysed in a homogenization buffer (50 mM Tris (pH 8.0), 150 mM NaCl, 5 mM EDTA, 1% Triton X-100) containing the following protease and phosphatase inhibitors: 10 μg/ml aprotinin, 25 μg/ml leupeptin, 10 μg/ml pepstatin, 10 μg/ml phenylmethanesulfonyl fluoride, 50 mM sodium fluoride, 50 mM sodium orthovanadate) for protein sample preparation. Cell viability determination[3] We determined cell viability by performing a lactate dehydrogenase (LDH) assay on the collected cell medium, as per the manufacturer’s instructions (Roche, Mannheim, Germany). LDH activities of control or baclofen-treated striatal cells were measured by absorbance at 490 nm. |
| Animal Protocol |
Animal/Disease Models: Wild type (WT) and mutant (MT) male YAC128 mice 13-18 months old [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. |
| References |
[1]. Mehdi Farokhnia, et al. A deeper insight into how GABA-B receptor agonism via baclofen may affect alcohol seeking and consumption: lessons learned from a human laboratory investigation. Mol Psychiatry. 2018 Oct 31.
[2]. Bexis, S., et al., Baclofen prevents MDMA-induced rise in core body temperature in rats. Drug Alcohol Depend, 2004. 74(1): p. 89-96. [3]. Woori Kim, et al. Baclofen, a GABAB receptor agonist, enhances ubiquitin-proteasome system functioning and neuronal survival in Huntington's disease model mice. Biochem Biophys Res Commun. 2014 Jan 10;443(2):706-11. |
| Molecular Formula |
C10H12CLNO2
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|---|---|
| Molecular Weight |
213.66
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| Exact Mass |
213.05566
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| Elemental Analysis |
C, 56.21; H, 5.66; Cl, 16.59; N, 6.56; O, 14.98
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| CAS # |
1134-47-0
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| Related CAS # |
(R)-Baclofen;69308-37-8;Baclofen-d4;1189938-30-4;(R)-Baclofen hydrochloride;63701-55-3;Baclofen hydrochloride;28311-31-1
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| Appearance |
White to off-white soild
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| LogP |
-1
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| tPSA |
63.3Ų
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| SMILES |
O=C(O)CC(C1=CC=C(Cl)C=C1)CN References
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| InChi Key |
KPYSYYIEGFHWSV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H12ClNO2/c11-9-3-1-7(2-4-9)8(6-12)5-10(13)14/h1-4,8H,5-6,12H2,(H,13,14)
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| Chemical Name |
4-amino-3-(4-chlorophenyl)butanoic acid
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| Synonyms |
Baclofen Lioresal, Liofen, Gablofen Baclon Kemstro
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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) |
DMSO : ~4.81 mg/mL (~22.51 mM)
H2O : ~2 mg/mL (~9.36 mM) 0.1 M HCL: ~10 mg/mL (~46.8 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (11.70 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
Solubility in Formulation 2: ~2.5 mg/mL (11.7 mM) in PBS (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6803 mL | 23.4017 mL | 46.8033 mL | |
| 5 mM | 0.9361 mL | 4.6803 mL | 9.3607 mL | |
| 10 mM | 0.4680 mL | 2.3402 mL | 4.6803 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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