Trimebutine maleate

Name: Trimebutine maleate
Brand: MedChemExpress
SKU: HY-B0380A
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0380A Purity: 99.91%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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 (BK_Ca 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.

Trimebutine maleate Chemical Structure

CAS No. : 34140-59-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Trimebutine maleate:

Trimebutine In-stock
Trimebutine-d₃ hydrochloride Get quote
Trimebutine maleate (Standard) Get quote

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Akt Isoform Specific Products:

View All Isoforms

Akt Akt1 Akt2 Akt3

View All Opioid Receptor Isoform Specific Products:

View All Isoforms

μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

View All NF-κB Isoform Specific Products:

View All Isoforms

NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All Calcium Channel Isoform Specific Products:

View All Isoforms

N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

View All Toll-like Receptor (TLR) Isoform Specific Products:

View All Isoforms

TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

View All IRAK Isoform Specific Products:

View All Isoforms

IRAK1 IRAK4

View All JNK Isoform Specific Products:

View All Isoforms

JNK1 JNK2 JNK3 JNK

View All ERK Isoform Specific Products:

View All Isoforms

ERK ERK1 ERK2 ERK5 ERK8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

μ Opioid Receptor/MOR

L-type calcium channel

IRAK-1

ERK1

ERK2

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:	SHG44, U251, U-87 MG
Concentration:	0, 10, 50, 100, 200 μM
Incubation Time:	48 h and 72 h
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).

In Vivo

Trimebutine (100 mg/kg/day; intraperitoneal injection; once a day; 7 days) maleate inhibits tumor growth in the subcutaneous xenograft model of U-87 MG glioma in female nude mice, increases TUNEL-positive apoptotic cells in tumor tissues, downregulates Bcl-2, upregulated Bax, and inhibits p-AKT and p-ERK signaling pathways^[1].
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.

Animal Model:	Female nude mice (4-week-old), subcutaneous U-87 MG glioblastoma xenograft model^[1]
Dosage:	100 mg/kg/day Trimebutine
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.
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.

Clinical Trial

Molecular Weight

503.54

Formula

C₂₆H₃₃NO₉

CAS No.

34140-59-5

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

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

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9859 mL	9.9297 mL	19.8594 mL
5 mM	0.3972 mL	1.9859 mL	3.9719 mL
10 mM	0.1986 mL	0.9930 mL	1.9859 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 (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.

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:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.96 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

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

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (286 KB) SDS (393 KB)

COA (258 KB) HNMR (270 KB) LCMS (95 KB)

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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.