2. GPCR/G Protein Apoptosis Stem Cell/Wnt Immunology/Inflammation PI3K/Akt/mTOR MAPK/ERK Pathway Neuronal Signaling NF-κB Membrane Transporter/Ion Channel
  3. Akt Opioid Receptor NF-κB Calcium Channel Potassium Channel Toll-like Receptor (TLR) IRAK Apoptosis JNK ERK
  4. Trimebutine

Trimebutine  (Synonyms: 曲美布汀)

目录号: HY-B0380 纯度: 99.42%
COA 产品使用指南 技术支持

Trimebutine 是一种多靶点抑制剂和阿片受体 (Opioid Receptor) 激动剂，具有抗毒蕈碱活性。Trimebutine 抑制 L 型钙通道 (L-type Ca2+ channels) 和大电导钙激活钾通道 (BKCa channels)，而抑制细胞外钙内流及钾离子外流。Trimebutine 还靶向 Toll 样受体，抑制 Toll-like receptor 2/4/7/8/9 信号而抑制 LPS 诱导 IRAK1 激活，以及 ERK1/2、JNK 和 NF-κB 的激活，从而发挥抗炎作用。Trimebutine 还通过抑制 AKT/ERK 通路诱导肿瘤细胞凋亡 (apoptosis)。Trimebutine 还抑制平滑肌过度收缩，可用于肠易激综合征 (IBS) 等胃肠道功能紊乱的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Trimebutine Chemical Structure

Trimebutine Chemical Structure

CAS No. : 39133-31-8

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥154
In-stock
50 mg ￥140
In-stock
100 mg ￥200
In-stock
500 mg ￥350
In-stock
1 g ￥500
In-stock
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

Trimebutine 相关抗体

Top Publications Citing Use of Products

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 Opioid Receptor 亚型特异性产品:

查看所有亚型
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 Calcium Channel 亚型特异性产品:

查看所有亚型
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

查看 Toll-like Receptor (TLR) 亚型特异性产品:

查看所有亚型
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

查看 IRAK 亚型特异性产品:

查看所有亚型
IRAK1 IRAK4

查看 JNK 亚型特异性产品:

查看所有亚型
JNK1 JNK2 JNK3 JNK

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

μ Opioid Receptor/MOR

 

L-type calcium channel

 

IRAK-1

 

ERK1

 

ERK2

 

体外研究
(In Vitro)

Trimebutine (0-1000 μM；48 h) 中可显著抑制 SHG44、U251、U-87 MG 胶质瘤细胞活力，IC50 分别为 98.28 μM、128.27 μM、204.06 μM，对正常 HEB 细胞毒性较低[1]。
Trimebutine (0-200 μM；24-72 h) 可抑制 U-87 MG 细胞迁移，呈浓度和时间依赖性[1]。
Trimebutine (0-200 μM；48-72 h) 可诱导胶质瘤细胞凋亡，下调 Bcl-2、上调 Bax 并激活 Caspase-3，同时抑制 AKT (Ser473) 和 ERK (Thr202/Tyr204) 磷酸化[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Trimebutine 相关抗体:

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).
体内研究
(In Vivo)

Trimebutine (100 mg/kg/day；腹腔注射；每天 1 次；7 d) 抑制雌性裸鼠 U-87 MG 胶质瘤皮下异种抑制模型的肿瘤生长，增加肿瘤组织中 TUNEL 阳性凋亡细胞，下调 Bcl-2、上调 Bax，并抑制 p-AKT 和 p-ERK 信号通路[1]。
Trimebutine (50 mg/kg；口服；单剂量) 处理 4 小时后，显著降低雄性小鼠结肠直肠扩张模型中 60 mmHg 压力下的痛觉反应，整体效果弱于等摩尔剂量的 GIC-1001 (HY-B0380B)[2]。

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
分子量

387.47

Formula

C22H29NO5
CAS 号
性状

固体

颜色

White to off-white

中文名称

曲美布汀
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

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

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (258.08 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5808 mL 12.9042 mL 25.8084 mL
5 mM 0.5162 mL 2.5808 mL 5.1617 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.42%

COA (288 KB) HNMR (268 KB) LCMS (99 KB)

产品使用指南 (1538 KB)
参考文献

Trimebutine 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trimebutine39133-31-8曲美布汀AktOpioid ReceptorNF-κBCalcium ChannelPotassium ChannelToll-like Receptor (TLR)IRAKApoptosisJNKERKPKBProtein kinase BNuclear factor-κBNuclear factor-kappaBCa2+ channelsCa channelsKcsAInterleukin-1 receptor associated kinaseIL-1R associated kinasec-Jun N-terminal kinaseExtracellular signal regulated kinasesInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
Trimebutine
目录号：
HY-B0380
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z