Baclofen
Based on 13 publication(s) in Google Scholar
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist with blood-brain barrier permeability. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
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- Pureza: 99.98%
- No. CAS: 1134-47-0
- Fòrmula: C10H12ClNO2
- Peso molecular:213.66
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) Baclofen
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
Actividad biológica
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | EC50 |
750 nM
Compound: baclofen
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Agonist activity at human recombinant GABABreceptor expressed in CHO-K1 cells assessed as inhibition of intracellular calcium release by FLIPR
Agonist activity at human recombinant GABABreceptor expressed in CHO-K1 cells assessed as inhibition of intracellular calcium release by FLIPR
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[PMID: 18578471] |
| HEK293 | EC50 |
1.7 μM
Compound: (+/-)-Baclofen
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Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay
Agonist activity at human GABA-B B1/B2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 3 hrs by luciferase reporter gene assay
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[PMID: 23428109] |
Baclofen (1, 10 μM; 24 h) 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.
Baclofen can cross the blood-brain barrier and cause depressive effects[4].
Note that the water solubility of Baclofen makes it difficult to cross the blood-brain barrier (BBB) ??after oral administration, so higher doses may be required in practice[5].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1134-47-0
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Appearance Solid
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Peso molecular 213.66
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Fòrmula C10H12ClNO2
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Color White to off-white
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SMILES
O=C(O)CC(C1=CC=C(Cl)C=C1)CN
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 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 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 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 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 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 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 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
Solvente y solubilidad
0.1 M HCl : 10 mg/mL (46.80 mM; Need ultrasonic)
DMSO : 4.76 mg/mL (22.28 mM; ultrasonic and warming and adjust pH to 4 with 1 M HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2 mg/mL (9.36 mM; Need ultrasonic)
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. 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. 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)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 2.5 mg/mL (11.70 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (480 KB)
- English - EN (480 KB)
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- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. 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 |
|---|---|---|---|---|---|
| H2O / DMSO / 0.1 M HCl | 1 mM | 4.6803 mL | 23.4017 mL | 46.8033 mL | 117.0083 mL |
| 5 mM | 0.9361 mL | 4.6803 mL | 9.3607 mL | 23.4017 mL | |
| DMSO / 0.1 M HCl | 10 mM | 0.4680 mL | 2.3402 mL | 4.6803 mL | 11.7008 mL |
| 15 mM | 0.3120 mL | 1.5601 mL | 3.1202 mL | 7.8006 mL | |
| 20 mM | 0.2340 mL | 1.1701 mL | 2.3402 mL | 5.8504 mL | |
| 0.1 M HCl | 25 mM | 0.1872 mL | 0.9361 mL | 1.8721 mL | 4.6803 mL |
| 30 mM | 0.1560 mL | 0.7801 mL | 1.5601 mL | 3.9003 mL | |
| 40 mM | 0.1170 mL | 0.5850 mL | 1.1701 mL | 2.9252 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.
Baclofen Related Classifications
HY-B0007 Related Classifications
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