Cat. No.: HY-B0007

Baclofen

13 Cited Publications

고객리뷰

Based on 13 publication(s) in Google Scholar

Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist with blood-brain barrier permeability. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.98%
CAS No.: 1134-47-0
화학식: C₁₀H₁₂ClNO₂
분자량:213.66

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Baclofen Chemical Structure

CAS No.: 1134-47-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	750 nM Compound: baclofen	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	[PMID: 18578471]
HEK293	EC₅₀	1.7 μM Compound: (+/-)-Baclofen	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	[PMID: 23428109]

In Vitro

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.

In Vivo

Baclofen (i.p.; 10 μg/g; twice daily for 3 consecutive days) ameliorates motor deficits in YAC128 HD transgenic mice^[3].
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.

Animal Model:

Wild type (WT) and mutant (MT) male YAC128 mice at 13-18 months of age^[3]
Dosage:

10 μg/g
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
Result:

Ameliorated motor deficits in YAC128 HD transgenic mice.
Increased proteasome activity and reduces neuronal intranuclear inclusions (NIIs) in YAC128 HD transgenic mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1134-47-0
Appearance Solid
분자량 213.66
화학식 C₁₀H₁₂ClNO₂
Color White to off-white
SMILES

O=C(O)CC(C1=CC=C(Cl)C=C1)CN
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (13)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyRT-PCRHistological Imaging/StainingWB

Sort by:

Journal Impact Factor

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]

GABA_B 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]

GABA_B receptor agonist (Baclofen, 0.25 µg/10 µL, i.t.) had no effect on chronic morphine tolerance.
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.
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 GABA_BR with Baclofen (10 mg/kg; i.p.; 7 days) strongly impaired the expression of GFAP in the ileum, as compared with the LPS group.
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

Baclofen Inhibits Glioma Proliferation via the MEK/ERK/CREB Pathway. [Abstract]

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

용액&용해도

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

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.

Protocol 1

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
H₂O / DMSO / 0.1 M HCl	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.

Keywords

Baclofen

13 Cited Publications

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Baclofen

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Publications Citing Use of MedChemExpress (MCE) Baclofen

Biological Activity

Chemical Information

Publications (13)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Baclofen Related Classifications

HY-B0007 Related Classifications