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Indomethacin

別名: Indometacin,NSC-77541 中文名稱：吲哚美辛

Indomethacin是一種非選擇性的COX1和COX2的抑制劑，IC50分別為0.1 μg/mL和5 μg/mL。常用于降低發(fā)熱、減緩疼痛、僵硬和腫脹。

Indomethacin Chemical Structure

Indomethacin Chemical Structure

CAS: 53-86-1

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 997 現(xiàn)貨
50mg 814.43 現(xiàn)貨
1g 3030.3 現(xiàn)貨
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Indomethacin相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

COX Signaling Pathways

COX信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述 Indomethacin是一種非選擇性的COX1和COX2的抑制劑，IC50分別為0.1 μg/mL和5 μg/mL。常用于降低發(fā)熱、減緩疼痛、僵硬和腫脹。
靶點(diǎn)
COX1 [6] COX-2 [6]
0.28 μM 14 μM
體外研究(In Vitro)
體外研究活性 Indomethacin以劑量依賴性方式抑制一種β-連環(huán)蛋白/ TCF響應(yīng)報(bào)道基因的轉(zhuǎn)錄。Indomethacin也下調(diào)了β-連環(huán)蛋白/ TCF轉(zhuǎn)錄針對(duì)細(xì)胞周期蛋白D1。Indomethacin通過(guò)調(diào)節(jié)TCF活動(dòng)而不破壞β-連環(huán)蛋白/ TCF復(fù)合物的形成減少β-連環(huán)蛋白/ TCF-應(yīng)答基因的轉(zhuǎn)錄。[1]
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 大鼠局灶性腦缺血后，Indomethacin增加所有細(xì)胞系的BrdU+細(xì)胞并減少小膠質(zhì)細(xì)胞/單核細(xì)胞活化。[2] Indomethacin（7.5 毫克/千克，1次注射）在遠(yuǎn)端空腸和回腸近端產(chǎn)生急性損傷和炎癥，在三天內(nèi)達(dá)到最大，一周內(nèi)完全解決。Indomethacin（每日2次皮下注射）產(chǎn)生一個(gè)更廣泛的和慢性炎癥，持續(xù)以活性形式存在于75％的大鼠中至少兩周。[3] 在SKH：HR-1-HRBR無(wú)毛小鼠中，Indomethacin（4ppm）減少腫瘤增產(chǎn)達(dá)78％。[4] Indomethacin（20 毫克/千克，口服）增加胃糜爛的總面積和大鼠的胃粘膜脂質(zhì)過(guò)氧化物的濃度。 Indomethacin增加α-生育酚：血清總膽固醇的比例。 Indomethacin抑制胃粘膜糜爛和脂質(zhì)過(guò)氧化物在胃粘膜的增加，血清α-生育酚的還原的減少。[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 --

化學(xué)信息&溶解度

分子量 357.79 分子式

C19H16ClNO4
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 72 mg/mL ( (201.23 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 24 mg/mL (67.07 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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