Baclofen hydrochloride
Based on 13 publication(s) in Google Scholar
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research.
For research use only. We do not sell to patients.
- Purity: 99.78%
- CAS No.: 28311-31-1
- Formula: C10H13Cl2NO2
- Molecular Weight:250.12
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Baclofen hydrochloride
More- Nat Neurosci. 2025 Jul;28(7):1404-1417. [Abstract]
- Cancer Res. 2023 Jul 5;83(13):2248-2261. [Abstract]
- Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]
- Biomed Pharmacother. 2025 Jan:182:117756. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Antioxidants (Basel). 2024 Sep 21;13(9):1141. [Abstract]
- Life Sci. 2023 Sep 15:329:121984. [Abstract]
- J Ovarian Res. 2020 Oct 24;13(1):126. [Abstract]
- FASEB J. 2020 Nov;34(11):14780-14798. [Abstract]
- Oncol Res. 2026 May 21;34(6):24. [Abstract]
- iScience. 2024 Jun 28;27(7):110415. [Abstract]
- Brain Res Bull. 2025 Jan 20:111217. [Abstract]
- eNeuro. 2025 Mar 7;12(3):ENEURO.0461-24.2025. [Abstract]
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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RT-PCR
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Cell Proliferation/Viability Assay
Biological Activity
Baclofen (1, 10 μM; 24 h) hydrochloride causes markedly decreased lactate dehydrogenase (LDH) activity, indicating increased cell viability in wild-type or mutant huntingtin-expressing striatal cells (HD19 or HD43). Baclofen significantly increases chymotrypsin-like proteasome activity and cell viability were in the HD43 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild type (WT) and mutant (MT) male YAC128 mice at 13-18 months of age[3]
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Dosage:10 μg/g
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Administration:IP; twice daily at 9:00 a.m. and 5:00 p.m., for 3 consecutive days; then single dose on the fourth day at 9:00 a.m
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Result:Ameliorated motor deficits in YAC128 HD transgenic mice.
Increased proteasome activity and reduces neuronal intranuclear inclusions (NIIs) in YAC128 HD transgenic mice.
Chemical Information
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CAS No. 28311-31-1
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Appearance Solid
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Molecular Weight 250.12
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Formula C10H13Cl2NO2
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Color White to off-white
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SMILES
O=C(CC(CN)C1=CC=C(C=C1)Cl)O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
GABA-dependent microglial elimination of inhibitory synapses underlies neuronal hyperexcitability in epilepsy. [Abstract]2025 Jul;28(7):1404-1417. PMID: 40425792 -
Cancer Res
Caffeine supplementation and FOXM1 inhibition enhance the antitumor effect of statins in neuroblastoma. [Abstract]2023 Jul 5;83(13):2248-2261. PMID: 37057874 -
Adv Sci (Weinh)
Morphine Tolerance Gated through EZH2-Mediated Suppression of Trpc5 in Spinal GABAergic Interneurons in Male Mice. [Abstract]2025 Oct 20:e07908. PMID: 41111460
Baclofen hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]
GABAB receptor agonist (Baclofen, 0.25 µg/10 µL, i.t.) had no effect on acute morphine analgesia.
Baclofen hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]
GABAB receptor agonist (Baclofen, 0.25 µg/10 µL, i.t.) had no effect on chronic morphine tolerance.
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Biomed Pharmacother
Identification of the atypical antipsychotic Asenapine as a direct survivin inhibitor with anticancer properties and sensitizing effects to conventional therapies. [Abstract]2025 Jan:182:117756. PMID: 39693907 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Antioxidants (Basel)
Activation of GABABR Attenuates Intestinal Inflammation by Reducing Oxidative Stress through Modulating the TLR4/MyD88/NLRP3 Pathway and Gut Microbiota Abundance. [Abstract]2024 Sep 21;13(9):1141. PMID: 39334800
Baclofen hydrochloride purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 Sep 21;13(9):1141. [Abstract]
Cell viability assessments were performed on IPEC-J2 cells in the CON, LPS, and LPS + Baclofen (100 μM; 12 h) groups.
Baclofen hydrochloride purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 Sep 21;13(9):1141. [Abstract]
The mRNA levels of IL-1β, IL-6, and TNF-α were measured by qRT-PCR in the CON, LPS, and LPS + Baclofen (100 μM; 12 h) groups. Baclofen pretreatment led to a considerable diminution in these proinflammatory factors, suggesting that activating GABABR in IPEC-J2 cells exerts anti-inflammatory actions.
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Life Sci
Activation of GABA receptor attenuates intestinal inflammation by modulating enteric glial cells function through inhibiting NF-κB pathway. [Abstract]2023 Sep 15:329:121984. PMID: 37527767
Baclofen hydrochloride purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Sep 15:329:121984. [Abstract]
Cell survival of EGCs after 3 h, 6 h, 12 h, 24 h incubation with control, GABA, Mus and Baclofen (100 μM) alone.
Baclofen hydrochloride purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Sep 15:329:121984. [Abstract]
Baclofen (10 mg/kg; i.p.; 7 days) noticeably attenuated ileum villous atrophy and inflammatory infiltration in mice challenge of LPS, while Baclofen alone had no obvious impact on ileal tissues.
Baclofen hydrochloride purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Sep 15:329:121984. [Abstract]
WB analysis showed the expression of GFAP. The results demonstrated that activation of GABABR with Baclofen (10 mg/kg; i.p.; 7 days) strongly impaired the expression of GFAP in the ileum, as compared with the LPS group.
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J Ovarian Res
Effects of activating GABAB1 receptor on proliferation, migration, invasion and epithelial-mesenchymal transition of ovarian cancer cells. [Abstract]2020 Oct 24;13(1):126. PMID: 33099319 -
FASEB J
Deficiency in the function of inhibitory interneurons contributes to glutamate-associated central sensitization through GABABR2-SynCAM1 signaling in chronic migraine rats. [Abstract]2020 Nov;34(11):14780-14798. PMID: 32931071 -
Oncol Res
2026 May 21;34(6):24. PMID: 42220433 -
iScience
Decoding sunitinib resistance in ccRCC: Metabolic-reprogramming-induced ABAT and GABAergic system shifts. [Abstract]2024 Jun 28;27(7):110415. PMID: 39100925 -
Brain Res Bull
GABAB receptors regulate the neural stem cell potential of Pkd2l1+ cerebrospinal fluid-contacting neurons via the PI3K/Akt signaling pathway. [Abstract]2025 Jan 20:111217. PMID: 39842645 -
eNeuro
Semicircular Canals Input Can Modify the Fast-Phase Nystagmus in Off-Vertical Axis Rotation of Mice. [Abstract]2025 Mar 7;12(3):ENEURO.0461-24.2025. PMID: 39993844
Solvent & Solubility
H2O : ≥ 100 mg/mL (399.81 mM)
DMSO : 10 mg/mL (39.98 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.9981 mL | 19.9904 mL | 39.9808 mL | 99.9520 mL |
| 5 mM | 0.7996 mL | 3.9981 mL | 7.9962 mL | 19.9904 mL | |
| 10 mM | 0.3998 mL | 1.9990 mL | 3.9981 mL | 9.9952 mL | |
| 15 mM | 0.2665 mL | 1.3327 mL | 2.6654 mL | 6.6635 mL | |
| 20 mM | 0.1999 mL | 0.9995 mL | 1.9990 mL | 4.9976 mL | |
| 25 mM | 0.1599 mL | 0.7996 mL | 1.5992 mL | 3.9981 mL | |
| 30 mM | 0.1333 mL | 0.6663 mL | 1.3327 mL | 3.3317 mL | |
| H2O | 40 mM | 0.1000 mL | 0.4998 mL | 0.9995 mL | 2.4988 mL |
| 50 mM | 0.0800 mL | 0.3998 mL | 0.7996 mL | 1.9990 mL | |
| 60 mM | 0.0666 mL | 0.3332 mL | 0.6663 mL | 1.6659 mL | |
| 80 mM | 0.0500 mL | 0.2499 mL | 0.4998 mL | 1.2494 mL | |
| 100 mM | 0.0400 mL | 0.1999 mL | 0.3998 mL | 0.9995 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.