Home Neuronal Signaling COX inhibitor Indomethacin For research use only.

Indomethacin

Synonyms: Indometacin,NSC-77541

Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling.

Indomethacin Chemical Structure

Indomethacin Chemical Structure

CAS No. 53-86-1

Purity & Quality Control

Indomethacin Related Products

Signaling Pathway

COX Signaling Pathways

COX Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
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
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
human 2008 cells Function assay Inhibition of human MRP1 in human 2008 cells, IC50=12 μM 18707884
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
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
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
Click to View More Cell Line Experimental Data

Biological Activity

Description Indomethacin is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling.
Targets
COX1 [6] COX-2 [6]
0.28 μM 14 μM
In vitro
In vitro Indomethacin inhibits transcription of a beta-catenin/TCF-responsive reporter gene in a dose dependent manner. Indomethacin also downregulates the beta-catenin/TCF transcriptional target cyclin D1. Indomethacin attenuates the transcription of beta-catenin/TCF-responsive genes, by modulating TCF activity without disrupting beta-catenin/TCF complex formation. [1]
In Vivo
In vivo Indomethacin increases BrdU+ cells of all lineages and reduces microglial/monocyte activation in rats after focal cerebral ischemia. [2] Indomethacin (7.5 mg/kg, one injection) produces acute injury and inflammation in the distal jejunum and proximal ileum that are maximal at three days and completely resolves within one week. Indomethacin (two daily subcutaneous injections) produces a more extensive and chronic inflammation that lasts in an active form in more than 75% of the rats for at least two weeks. [3] Indomethacin (4ppm) reduces tumor yield by 78% in SKH:HR-1-hrBr hairless mice. [4] Indomethacin (20 mg/kg, orally) increases the total area of gastric erosions and concentration of lipid peroxides in the gastric mucosa of rats. Indomethacin increases the alpha-tocopherol:total cholesterol ratio in serum. Indomethacin inhibits the increases in gastric mucosal erosions and lipid peroxides in the gastric mucosa, and the reduction of serum alpha-tocopherol. [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 --

Chemical Information & Solubility

Molecular Weight 357.79 Formula

C19H16ClNO4
CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (201.23 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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