Art. -Nr.: HY-B0380

Trimebutine

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Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine 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 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 also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

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Reinheit: 99.42%
CAS. Nr.: 39133-31-8
Formel: C₂₂H₂₉NO₅
Molecular Weight:387.47

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Trimebutine Chemical Structure

CAS. Nr.: 39133-31-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

μ Opioid Receptor/MOR

L-type calcium channel

IRAK-1

ERK1

ERK2

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

Alle JNK Isoform-spezifische Produkte anzeigen :

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen :

Alle IRAK Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

In Vitro

Trimebutine (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 (0-200 μM; 24-72 h) inhibits the migration of U-87 MG cells in a concentration- and time-dependent manner^[1].
Trimebutine (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.

Cell Viability Assay^[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) 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) 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:
Dosage:
Administration:
Result:

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

Animal Model:

Female nude mice (4-week-old), subcutaneous U-87 MG glioblastoma xenograft model^[1]
Dosage:

100 mg/kg/day
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

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

Chemical Information

CAS. Nr. 39133-31-8
Appearance Solid
Molecular Weight 387.47
Formel C₂₂H₂₉NO₅
Color White to off-white
SMILES

O=C(OCC(C1=CC=CC=C1)(N(C)C)CC)C2=CC(OC)=C(OC)C(OC)=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (258.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.5808 mL

12.9042 mL

25.8084 mL

5 mM

0.5162 mL

2.5808 mL

5.1617 mL

10 mM

0.2581 mL

1.2904 mL

2.5808 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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)

Verweise

[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]. 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]

[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]. 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]

[5]. 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]

[6]. 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]

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5808 mL	12.9042 mL	25.8084 mL	64.5211 mL
	5 mM	0.5162 mL	2.5808 mL	5.1617 mL	12.9042 mL
	10 mM	0.2581 mL	1.2904 mL	2.5808 mL	6.4521 mL
	15 mM	0.1721 mL	0.8603 mL	1.7206 mL	4.3014 mL
	20 mM	0.1290 mL	0.6452 mL	1.2904 mL	3.2261 mL
	25 mM	0.1032 mL	0.5162 mL	1.0323 mL	2.5808 mL
	30 mM	0.0860 mL	0.4301 mL	0.8603 mL	2.1507 mL
	40 mM	0.0645 mL	0.3226 mL	0.6452 mL	1.6130 mL
	50 mM	0.0516 mL	0.2581 mL	0.5162 mL	1.2904 mL
	60 mM	0.0430 mL	0.2151 mL	0.4301 mL	1.0754 mL
	80 mM	0.0323 mL	0.1613 mL	0.3226 mL	0.8065 mL
	100 mM	0.0258 mL	0.1290 mL	0.2581 mL	0.6452 mL

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Trimebutine

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