メタキサロン
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.77%
- CAS 番号: 1665-48-1
- 分子式: C12H15NO3
- 分子量:221.26
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
生物活性
PPARγ and MAO-A[1]
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.
-
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 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 1665-48-1
-
性状 Solid
-
分子量 221.26
-
分子式 C12H15NO3
-
Color White to off-white
-
SMILES
O=C1OC(COC2=CC(C)=CC(C)=C2)CN1
-
別名
Metaxalone; AHR438; NSC170959
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (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)
-
取扱説明書 (2659 KB)
参考文献
[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]
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, 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 |