生物活性：Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate 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 fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate 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][7].
IC50 & Target：μ Opioid Receptor/MOR
L-type calcium channel
IRAK-1
ERK1
ERK2
体外研究(In Vitro)：氢、碳和其他元素的稳定重同位素已被掺入药物分子中，主要用作药物研发过程中定量分析的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而备受关注[1]。
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Trimebutine-d5 fumarate 相关抗体:
Annexin VI Antibody
ERK1/2 Antibody
Phospho-ERK1/2 (Thr202/Tyr204)/(Thr185/Tyr187) Antibody
NF-KB p65 Antibody
Phospho-ERK1/2 (Thr202/Tyr204)/(Thr185/Tyr187) Antibody (YA455)
Phospho-NF-KB p65 (Ser536) Antibody
E-Cadherin Antibody (YA470)
IRF3 Antibody
Fatty Acid Synthase Antibody (YA766)
Phospho-AKT1 (Ser473) Antibody
AKT1/2/3 Antibody (YA633)
DYKDDDDK Tag (FLAG) Antibody
GAPDH Antibody
GFP Antibody
p53 Antibody (YA250)
RUNX2 Antibody
Phospho-NF-κB p65 (Ser529) Antibody
Ferritin Heavy Chain Antibody
JNK Antibody
Phospho-AKT (Thr308) Antibody
Toll-Like Receptor 4 Antibody
COX2 Antibody
Ctip2 Antibody
Cyclin D1 Antibody (YA485)
Cytochrome C Antibody
NF-KB p65 Antibody (YA267)
Phospho-AKT1(Ser473) Antibody
ERK2 Antibody
c-Myc Antibody
Cyclin E1 Antibody
分子量：508.57
Formula：C26H28D5NO9
CAS 号：2747915-18-8
非标记 CAS：39133-31-8
中文名称：曲美布汀-d5
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (545 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
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[2]. Fan YP, et al. Trimebutine Promotes Glioma Cell Apoptosis as a Potential Anti-tumor Agent. Front Pharmacol. 2018 Jun 21;9:664.
 [Content Brief]
[3]. 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.
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[4]. 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]
[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]
[7]. 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]