Name: Indomethacin
Brand: Selleck Chemicals
SKU: S1723
Rating: 5 (16 reviews)

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

CAS: 53-86-1

Selleck's Indomethacin has been cited by 16 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 100.00%

100.00

Indomethacin Related Products

Related Targets	COX-1 COX-2	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Anti-alzheimer Disease Compound Library	Click to Expand

Signaling Pathway

COX Signaling Pathway

Choose Selective COX Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06031363	Recruiting	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	--

References

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Batch:

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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.

Handling Instructions

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