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Trimebutine

CAT: 0804-HY-B0380-01Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-B0380-01Size:500 mg
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Description
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 (BKCa 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) [1][2][3][4][5][6].
CAS Number
39133-31-8
UNSPSC
12352005
Hazard Statement
H302, H312, H332, H413
Target
Akt; Apoptosis; Calcium Channel; ERK; IRAK; JNK; NF-κB; Opioid Receptor; Potassium Channel; Toll-like Receptor (TLR)
Type
Reference compound
Related Pathways
Apoptosis; GPCR/G Protein; Immunology/Inflammation; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Neuronal Signaling; NF-κB; PI3K/Akt/mTOR; Stem Cell/Wnt
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Cancer; Metabolic Disease; Inflammation/Immunology; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/trimebutine.html
Concentration
10mM
Purity
99.42
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(OCC(C1=CC=CC=C1)(N(C)C)CC)C2=CC(OC)=C(OC)C(OC)=C2
Molecular Formula
C22H29NO5
Molecular Weight
387.47
Precautions
H302, H312, H332, H413
References & Citations
[1]Fan YP, et al. Trimebutine Promotes Glioma Cell Apoptosis as a Potential Anti-tumor Agent. Front Pharmacol. 2018 Jun 21;9:664.|[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.|[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.|[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.|[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.|[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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
ERK1; ERK2; IRAK1; L-type calcium channel; μ Opioid Receptor/MOR

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B1650-STrimebutine
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CS-O-31919Trimebutine - Impurity A

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