Cat. No.: HY-B0678

Metaxalone

(Synonyms: AHR438; NSC170959)

Customer Review

Based on 1 Customer Validation

Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia.

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

Purity: 99.77%
CAS No.: 1665-48-1
Formula: C₁₂H₁₅NO₃
Molecular Weight:221.26

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Metaxalone Chemical Structure

CAS No.: 1665-48-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PPARγ and MAO-A^[1]

All NF-κB Isoforms :

In Vitro

Metaxalone (10-40 µg/mL; 1 h) reverses the inflammatory phenotype of IL-1β-treated HMC3 cells, decreases the expression of pro-inflammatory factors TNF-α and IL-6, and increases the expression of anti-inflammatory factor IL-13^[1].
Metaxalone (10-40 µg/mL; 1 h) shows antioxidant properties in IL-1β-treated HMC3 cells, significantly upregating Nrf2 levels and decreasing MDA levels^[1].
Metaxalone (10-40 µg/mL; 1 h) inhibits the increase of NF-κB and stimulates the activation of PPARγ and PGC-1α in IL-1β-treated HMC3 cells^[1].
Metaxalone (10-40 µg/mL; 1 h) inhibits MAO-A activity in a dose-dependent manner^[1].
Metaxalone (10-40 µg/mL; 24-72 h) has no cytotoxic effect on HMC3 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

IL-1β treated human microglial HMC3 cell line
Concentration:

10, 20, and 40 µg/mL
Incubation Time:

1 h
Result:

Increased the levels of Nrf2 in a concentration‐dependent manner.

Cell Viability Assay^[1]

Cell Line:

Human microglial HMC3 cell line
Concentration:

10, 20, and 40 µg/mL
Incubation Time:

24, 48 and 72 h
Result:

Did not produce any toxic effect in the treated cells and related viability percentage kept similar to control.

Clinical Trial

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

Chemical Information

CAS No. 1665-48-1
Appearance Solid
Molecular Weight 221.26
Formula C₁₂H₁₅NO₃
Color White to off-white
SMILES

O=C1OC(COC2=CC(C)=CC(C)=C2)CN1
Synonyms

AHR438; NSC170959
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (451.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

4.5197 mL

22.5983 mL

45.1965 mL

5 mM

0.9039 mL

4.5197 mL

9.0393 mL

10 mM

0.4520 mL

2.2598 mL

4.5197 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (11.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (11.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (11.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
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]. Pallio G, D'Ascola A, Cardia L, et al. MAO-A Inhibition by Metaxalone Reverts IL-1β-Induced Inflammatory Phenotype in Microglial Cells. Int J Mol Sci. 2021;22(16):8425. [Content Brief]

[2]. Stanko JR. Review of oral skeletal muscle relaxants for the craniomandibular disorder (CMD) practitioner. Cranio. 1990 Jul;8(3):234-43. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.5197 mL	22.5983 mL	45.1965 mL	112.9913 mL
	5 mM	0.9039 mL	4.5197 mL	9.0393 mL	22.5983 mL
	10 mM	0.4520 mL	2.2598 mL	4.5197 mL	11.2991 mL
	15 mM	0.3013 mL	1.5066 mL	3.0131 mL	7.5328 mL
	20 mM	0.2260 mL	1.1299 mL	2.2598 mL	5.6496 mL
	25 mM	0.1808 mL	0.9039 mL	1.8079 mL	4.5197 mL
	30 mM	0.1507 mL	0.7533 mL	1.5066 mL	3.7664 mL
	40 mM	0.1130 mL	0.5650 mL	1.1299 mL	2.8248 mL
	50 mM	0.0904 mL	0.4520 mL	0.9039 mL	2.2598 mL
	60 mM	0.0753 mL	0.3766 mL	0.7533 mL	1.8832 mL
	80 mM	0.0565 mL	0.2825 mL	0.5650 mL	1.4124 mL
	100 mM	0.0452 mL	0.2260 mL	0.4520 mL	1.1299 mL

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Metaxalone

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All NF-κB Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Metaxalone Related Classifications

HY-B0678 Related Classifications