Indomethacin
别名: Indometacin,NSC-77541 中文名称：吲哚美辛
Indomethacin是一种非选择性的COX1和COX2的抑制剂，IC50分别为0.1 μg/mL和5 μg/mL。常用于降低发热、减缓疼痛、僵硬和肿胀。
Indomethacin Chemical Structure
CAS: 53-86-1
产品质控
批次：
纯度：
99.99%
99.99
Indomethacin相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| THP1 cells | Function assay | 100 μM | 30 mins | Irreversible inhibition of COX-1 in human THP1 cells assessed as inhibition of arachidonic acid-induced TXB2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay | 23651359 |
| MDA-MB-231 cells | Function assay | 100 μM | 30 mins | Irreversible inhibition of COX-1 in human MDA-MB-231 cells assessed as inhibition of arachidonic acid-induced PGE2 formation at 100 uM incubated for 30 mins followed by compound washout measured 30 mins post arachidonic acid challenge by radioimmunoassay | 23651359 |
| LNCAP cells | Function assay | 30 μM | 48 h | Inhibition of AKR1C3 (unknown origin)-mediated testosterone-17beta-glucuronide formation expressed in human LNCAP cells at 30 uM after 48 hrs in presence of 4-androstene-3,17-dione | 23432095 |
| A549 cells | Function assay | 10 μM | Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 10 uM by cell-intact assay | 19053751 | |
| HepG2 cells | Function assay | 100 μM | Inhibition of MRP1-mediated doxorubicin efflux in doxorubicin resistant human HepG2 cells at 100 uM by flow cytometry | 20455578 | |
| HeLa cells | Function assay | 20 mins | Agonist activity at androgen receptor (unknown origin) expressed in HeLa cells co-expressing PSA-(ARE)4-Luc13 assessed as induction of DHT-induced luciferase activity after 20 mins by luciferase reporter gene assay, EC50=0.14 nM | 23432095 | |
| SF-9 insect cells | Function assay | 20 Mins | Inhibition of human COX2 expressed in SF-9 insect cells assessed as conversion of [14C]-arachidonic acid to [14C]-prostaglandins preincubated for 20 mins by thin-layer chromatography analysis, IC50=0.75 μM | 21524587 | |
| mouse RAW264.7 cells | Function assay | 24 h | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess assay, IC50=1.25 μM | 24806310 | |
| mouse BV2 cells | Function assay | 24 h | Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess assay, IC50=7.1 μM | 24042007 | |
| mouse BV2 cells | Cytotoxicity assay | 24 h | Cytotoxicity against mouse BV2 cells assessed as maximum non-toxic concentration after 24 hrs by MTT assay | 23711917 | |
| J774 cells | Function assay | In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells, IC50=2 nM | 15857149 | ||
| U-937 cells | Function assay | In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells, IC50=2 nM | 12877584 | ||
| rat synovial cells | Function assay | In vitro inhibitory effect on production of prostaglandin E2 (PGE2) in rat synovial cells, IC50=2.9 nM | 10821716 | ||
| 143982 cells | Function assay | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells, IC50=9 nM | 12877584 | ||
| CHO cells | Function assay | In vitro inhibitory potency against human COX-1 in stably transfected chinese hamster ovary (CHO) cells, IC50=18 nM | 10576684 | ||
| RBL-1 cell line | Function assay | Inhibition of Prostaglandin G/H synthase in intact RBL-1 cell line, IC50=0.5 μM | 2115586 | ||
| human 2008 cells | Function assay | Inhibition of human MRP1 in human 2008 cells, IC50=12 μM | 18707884 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Indomethacin是一种非选择性的COX1和COX2的抑制剂，IC50分别为0.1 μg/mL和5 μg/mL。常用于降低发热、减缓疼痛、僵硬和肿胀。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Indomethacin以剂量依赖性方式抑制一种β-连环蛋白/ TCF响应报道基因的转录。Indomethacin也下调了β-连环蛋白/ TCF转录针对细胞周期蛋白D1。Indomethacin通过调节TCF活动而不破坏β-连环蛋白/ TCF复合物的形成减少β-连环蛋白/ TCF-应答基因的转录。[1] | |||
|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | 大鼠局灶性脑缺血后，Indomethacin增加所有细胞系的BrdU+细胞并减少小胶质细胞/单核细胞活化。[2] Indomethacin（7.5 毫克/千克，1次注射）在远端空肠和回肠近端产生急性损伤和炎症，在三天内达到最大，一周内完全解决。Indomethacin（每日2次皮下注射）产生一个更广泛的和慢性炎症，持续以活性形式存在于75％的大鼠中至少两周。[3] 在SKH：HR-1-HRBR无毛小鼠中，Indomethacin（4ppm）减少肿瘤增产达78％。[4] Indomethacin（20 毫克/千克，口服）增加胃糜烂的总面积和大鼠的胃粘膜脂质过氧化物的浓度。 Indomethacin增加α-生育酚：血清总胆固醇的比例。 Indomethacin抑制胃粘膜糜烂和脂质过氧化物在胃粘膜的增加，血清α-生育酚的还原的减少。[5] | |
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06031363 | Completed | Pancreatitis|Cholangiopancreatography Endoscopic Retrograde|Indomethacin |
The First Affiliated Hospital of Soochow University |
November 1 2022 | Not Applicable |
| NCT04821323 | Completed | Healthy |
Janssen Research & Development LLC |
March 10 2021 | Early Phase 1 |
| NCT04025177 | Withdrawn | Patent Ductus Arteriosus After Premature Birth |
University of Manitoba|St. Boniface Hospital|Health Sciences Centre Winnipeg Manitoba|University at Buffalo |
January 2020 | Phase 2 |
| NCT03967483 | Unknown status | Headache Migraine |
Anne Ducros|French Society for the Study of Migraine Headache |
June 1 2019 | -- |
化学信息&溶解度
| 分子量 | 357.79 | 分子式 | C19H16ClNO4 |
| CAS号 | 53-86-1 | SDF | Download Indomethacin SDF |
| Smiles | CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 72 mg/mL ( (201.23 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 24 mg/mL (67.07 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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