Trimebutine maleate
Based on 1 Customer Validation
Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 34140-59-5
- Formula: C26H33NO9
- Molecular Weight:503.54
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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μ Opioid Receptor/MOR |
L-type calcium channel |
IRAK-1 |
ERK1 |
ERK2 |
Trimebutine maleate (0-1000 μM; 48 h) significantly inhibits the viability of SHG44, U251, and U-87 MG glioma cells, with IC50 of 98.28 μM, 128.27 μM, and 204.06 μM, respectively, and has low toxicity to normal HEB cells[1].
Trimebutine maleate (0-200 μM; 24-72 h) inhibits the migration of U-87 MG cells in a concentration- and time-dependent manner[1].
Trimebutine maleate (0-200 μM; 48-72 h) induces apoptosis in glioma cells, downregulates Bcl-2, upregulates Bax and activates Caspase-3, while inhibiting the phosphorylation of AKT (Ser473) and ERK (Thr202/Tyr204)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SHG44, U251, U-87 MG
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Concentration:0, 10, 50, 100, 200 μM
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Incubation Time:48 h and 72 h
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Result:Reduced phosphorylated AKT (Ser473) and ERK (Thr202/Tyr204) levels in a dose-dependent manner at both time points, while total AKT and ERK protein levels remained unchanged.
The inhibition was more pronounced at 72 h for higher concentrations (100-200 μM).
Trimebutine (50 mg/kg; oral; single dose) maleate significantly reduces pain response at 60 mmHg pressure in the colorectal distension model of male mice after 4 hours of treatment, exhibits weaker overall effect than GIC-1001 (HY-B0380B) at an equimolar dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (4-week-old), subcutaneous U-87 MG glioblastoma xenograft model[1]
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Dosage:100 mg/kg/day Trimebutine
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Administration:Intraperitoneal injection (i.p.), once daily for 7 days, starting when tumors reached ~2 mm3; monitored at days 7, 10, 14, 16, 18, 21.
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Result:Significantly reduced tumor volume compared to the vehicle control group, with final tumor weight decreasing by ~30%. Histological analysis showed increased TUNEL-positive apoptotic cells in tumor sections.
Downregulated Bcl-2 and upregulated Bax protein levels, along with reduced phosphorylation of AKT (Ser473) and ERK (Thr202/Tyr204), indicating modulation of apoptotic and proliferative signaling pathways.
No significant toxicity was observed in treated mice, as body weight and general activity remained comparable to controls.
Chemical Information
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CAS No. 34140-59-5
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Appearance Solid
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Molecular Weight 503.54
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Formula C26H33NO9
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Color White to off-white
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SMILES
O=C(O)/C=C\C(O)=O.O=C(OCC(C1=CC=CC=C1)(N(C)C)CC)C2=CC(OC)=C(OC)C(OC)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (198.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (49.65 mM; Need ultrasonic)
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 (sealed storage, away from moisture). 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.
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 (sealed storage, away from moisture). 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (4.96 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 (4.96 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Fan YP, et al. Trimebutine Promotes Glioma Cell Apoptosis as a Potential Anti-tumor Agent. Front Pharmacol. 2018 Jun 21;9:664. [Content Brief]
[2]. Tan W, et al. Effects of trimebutine maleate on colonic motility through Ca²+-activated K+ channels and L-type Ca²+ channels. Arch Pharm Res. 2011 Jun;34(6):979-85. [Content Brief]
[3]. Long Y, et al. Effectiveness of trimebutine maleate on modulating intestinal hypercontractility in a mouse model of postinfectious irritable bowel syndrome. Eur J Pharmacol. 2010 Jun 25;636(1-3):159-65. [Content Brief]
[4]. Xu J, et al. Trimebutine, a small molecule mimetic agonist of adhesion molecule L1, contributes to functional recovery after spinal cord injury in mice. Dis Model Mech. 2017 Sep 1;10(9):1117-1128. [Content Brief]
[5]. Ogawa N, et al. Trimebutine suppresses Toll-like receptor 2/4/7/8/9 signaling pathways in macrophages. Arch Biochem Biophys. 2021 Oct 30;711:109029. [Content Brief]
[6]. Cenac N, et al. A novel orally administered trimebutine compound (GIC-1001) is anti-nociceptive and features peripheral opioid agonistic activity and Hydrogen Sulphide-releasing capacity in mice. Eur J Pain. 2016 May;20(5):723-30. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 |
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| H2O / DMSO | 1 mM | 1.9859 mL | 9.9297 mL | 19.8594 mL | 49.6485 mL |
| 5 mM | 0.3972 mL | 1.9859 mL | 3.9719 mL | 9.9297 mL | |
| 10 mM | 0.1986 mL | 0.9930 mL | 1.9859 mL | 4.9648 mL | |
| 15 mM | 0.1324 mL | 0.6620 mL | 1.3240 mL | 3.3099 mL | |
| 20 mM | 0.0993 mL | 0.4965 mL | 0.9930 mL | 2.4824 mL | |
| 25 mM | 0.0794 mL | 0.3972 mL | 0.7944 mL | 1.9859 mL | |
| 30 mM | 0.0662 mL | 0.3310 mL | 0.6620 mL | 1.6549 mL | |
| 40 mM | 0.0496 mL | 0.2482 mL | 0.4965 mL | 1.2412 mL | |
| DMSO | 50 mM | 0.0397 mL | 0.1986 mL | 0.3972 mL | 0.9930 mL |
| 60 mM | 0.0331 mL | 0.1655 mL | 0.3310 mL | 0.8275 mL | |
| 80 mM | 0.0248 mL | 0.1241 mL | 0.2482 mL | 0.6206 mL | |
| 100 mM | 0.0199 mL | 0.0993 mL | 0.1986 mL | 0.4965 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.
Trimebutine maleate Related Classifications
HY-B0380A Related Classifications
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