Baclofen

Name: Baclofen
Brand: MedChemExpress
SKU: HY-B0007
Rating: 5.0 (12 reviews)

Cat. No.: HY-B0007 Purity: 99.98%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 1134-47-0

Size	Stock	Quantity
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	Get quote
50 g	Get quote

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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Baclofen:

12 Publications Citing Use of MCE Baclofen

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

RT-PCR

Histological Imaging/Staining

: 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.

: Baclofen purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 Sep 21;13(9):1141.; 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.; 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.

: 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.

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References
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Description

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

Molecular Weight

213.66

Formula

C₁₀H₁₂ClNO₂

CAS No.

1134-47-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC(C1=CC=C(Cl)C=C1)CN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (276 KB) SDS (480 KB)

COA (249 KB) HNMR (118 KB) RP-HPLC (224 KB) LCMS (230 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]

Complete Stock Solution Preparation Table

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.

Baclofen Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Baclofen1134-47-0GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorLipophilicγ-aminobutyric acidGABAorallyGABABRblood brain barrierbbbspasticityInhibitorinhibitorinhibit

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Baclofen

Customer Review

Other Forms of Baclofen:

Baclofen Related Antibodies

12 Publications Citing Use of MCE Baclofen

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•Related Screening Libraries:

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•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Baclofen Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

Baclofen Related Classifications

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