2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Baclofen

Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. 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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Baclofen Chemical Structure

Baclofen Chemical Structure

CAS No. : 1134-47-0

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Based on 6 publication(s) in Google Scholar

Other Forms of Baclofen:

Baclofen Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. 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[1][2][3].

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.

Baclofen Related Antibodies
In Vivo

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

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.
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 : 4.81 mg/mL (22.51 mM; ultrasonic and warming and adjust pH to 4 with 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
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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

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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)

g

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: 99.87%

COA (249 KB) LCMS (86 KB)

Handling Instructions (2659 KB)
References

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.

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Baclofen Related Classifications

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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