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Indomethacin COX inhibitor

Cat.No.S1723

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.
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Quality Control

Batch: Purity: 100.00%
100.00

Cell Culture, Treatment & Working Concentration

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
J774 cells Function assay In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells, IC50=2 nM
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
rat synovial cells Function assay In vitro inhibitory effect on production of prostaglandin E2 (PGE2) in rat synovial cells, IC50=2.9 nM
143982 cells Function assay In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells, IC50=9 nM
CHO cells Function assay In vitro inhibitory potency against human COX-1 in stably transfected chinese hamster ovary (CHO) cells, IC50=18 nM
RBL-1 cell line Function assay Inhibition of Prostaglandin G/H synthase in intact RBL-1 cell line, IC50=0.5 μM
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
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
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
human 2008 cells Function assay Inhibition of human MRP1 in human 2008 cells, IC50=12 μM
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
HepG2 cells Function assay 100 μM Inhibition of MRP1-mediated doxorubicin efflux in doxorubicin resistant human HepG2 cells at 100 uM by flow cytometry
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
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
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
mouse BV2 cells Cytotoxicity assay 24 h Cytotoxicity against mouse BV2 cells assessed as maximum non-toxic concentration after 24 hrs by MTT assay
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Solubility

In vitro
Batch:

DMSO : 72 mg/mL (201.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 357.79 Formula

C19H16ClNO4

Storage (From the date of receipt)
CAS No. 53-86-1 Download SDF Storage of Stock Solutions

Synonyms Indometacin,NSC-77541 SMILES CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)O

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
COX1
0.28 μM
COX-2
14 μM
In vitro
Indomethacin inhibits transcription of a beta-catenin/TCF-responsive reporter gene in a dose dependent manner. This compound also downregulates the beta-catenin/TCF transcriptional target cyclin D1. It attenuates the transcription of beta-catenin/TCF-responsive genes, by modulating TCF activity without disrupting beta-catenin/TCF complex formation.
In vivo
Indomethacin increases BrdU+ cells of all lineages and reduces microglial/monocyte activation in rats after focal cerebral ischemia. This compound (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. It (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. This chemical (4ppm) reduces tumor yield by 78% in SKH:HR-1-hrBr hairless mice. It (20 mg/kg, orally) increases the total area of gastric erosions and concentration of lipid peroxides in the gastric mucosa of rats. This compound increases the alpha-tocopherol:total cholesterol ratio in serum. It inhibits the increases in gastric mucosal erosions and lipid peroxides in the gastric mucosa, and the reduction of serum alpha-tocopherol.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10449029/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8314503/
  • [6] https://pubmed.ncbi.nlm.nih.gov/8265610/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07661498 NOT_YET_RECRUITING
Pancreatitis Biliary; Pancreatitis Acute Biliary; Pancreatitis; Post-ERCP Pancreatitis; Post-ERCP Acute Pancreatitis; Post-ERCP Adverse Events
University of California, San Francisco
2026-07 PHASE4
NCT07218653 NOT_YET_RECRUITING
Metabolic Syndrome
University of Wisconsin, Madison
2026-09 EARLY_PHASE1
NCT00262470 ACTIVE_NOT_RECRUITING
Tachycardia; Chronic Orthostatic Intolerance
Satish R. Raj
1997-04 PHASE1; PHASE2
NCT07330284 RECRUITING
Pancreatitis; ERCP Surgery
University of Kansas Medical Center
2025-12-05
NCT07560566 RECRUITING
Hepato Cellular Carcinoma (HCC); Hand Foot Skin Syndrome
National Taiwan University Hospital
2025-12-09 PHASE2
NCT06572917 NOT_YET_RECRUITING
Extreme Prematurity; Intraventricular Hemorrhage; Morbidity;Newborn
University of British Columbia
2025-11-01 PHASE2

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