Trimebutine Maleate is an agonist effect on peripheral μ, k and δ opiate receptors, and also shows antimuscarinic effect.
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产品名称 | Opioid receptor ↓ ↑ | ORL1 ↓ ↑ | μ-opioid receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Racecadotril | ✔ | 98% | |||||||||||||||||
JTC-801 |
++
Opioid receptor-like1 (ORL1), IC50: 94 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Trimebutine maleate is an orally administered anti-tumor agent. It has the ability to selectively inhibit the stemness and proliferation of ovarian cancer stem cells (CSCs). Additionally, Trimebutine maleate alleviates colonic muscle hypercontractility, regulates gastrointestinal motility, and promotes apoptosis, making it a valuable candidate for research in glioma/glioblastoma and irritable bowel syndrome[1].[2].[3].[4].[5].[6]. |
体内研究 | Furthermore, when administered orally at doses of 25-50 mg/kg in a single dose, Trimebutine maleate lessens the response to colorectal distension in C57Bl6 male mice, indicating its potential effectiveness in addressing gastrointestinal discomfort[4]. |
体外研究 | In vitro, Trimebutine maleate (1-20 μM, 60 h) has been shown to reduce the growth of A2780-SP cells dose-dependently[2]. Trimebutine maleate (1-10 μM, 24 h) also diminishes stem cell characteristics of A2780-SP cells by concurrently inhibiting calcium and BKCa channels[2]. For glioma and glioblastoma cells, Trimebutine maleate (10-200 μM, 24-72 h) not only reduces cell viability and migration but also obstructs the ERK and AKT signaling pathways, which are critical for cell proliferation and survival[3]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01507922 | Irritable Bowel Syndrome | Phase 4 | Completed | - | Korea, Republic of ... 展开 >> Korea University Ansan Hospital Ansan, Korea, Republic of Hallym University Sacred Heart Hospital Anyang, Korea, Republic of Kangwon National University Hospital Chuncheon, Korea, Republic of Gachon University Gil Hospital Incheon, Korea, Republic of Inje University Seoul Paik Hospital Seoul, Korea, Republic of Korea University Anam Hospital Seoul, Korea, Republic of Korea University Guro Hospital Seoul, Korea, Republic of 收起 << |
NCT02986685 | Refractory Reflux Esophagitis | Phase 4 | Unknown | November 2017 | China, Shaanxi ... 展开 >> Xijing Hosipital of Digestive Disease Recruiting Xi`an, Shaanxi, China, 710032 Contact: Yongquan Shi, professor 86-029-84771515 shiyquan@fmmu.edu.cn 收起 << |
NCT01984931 | Nausea Vomiti... 展开 >>ng 收起 << | Phase 3 | Unknown | December 2013 | Korea, Republic of ... 展开 >> Chungmu General Hopsital Recruiting Seoul, Yeongdeungpo-gu, Korea, Republic of, 150-034 Contact: Sang Hoon Lhee, MD, Phd +82 (2) 2068/4525 cmirb@naver.com Principal Investigator: Paolo Alan B Tabar, MD 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.93mL 1.99mL 0.99mL |
19.86mL 3.97mL 1.99mL |
CAS号 | 34140-59-5 |
分子式 | C26H33NO9 |
分子量 | 503.541 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(208.52 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 25 mg/mL(49.65 mM),配合低频超声助溶 |
动物实验配方 |