Name: Indomethacin
Brand: Selleck Chemicals
SKU: S1723
Availability: InStock
Rating: 5 (21 reviews)

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Quality Control

Batch: Purity: 100.00%

100.00

Related Targets	Adrenergic Receptor AChR 5-HT Receptor Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other COX Inhibitors	NS-398 (NS398) Paeoniflorin (NSC 178886) Lumiracoxib Xanthohumol Bufexamac Oroxin B Tolfenamic Acid Nimesulide Ginsenoside Rd Indometacin Sodium

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
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
Click to View More Cell Line Experimental Data

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 30%PEG300 2 5%Tween80 3 60%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (5.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 600 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	357.79	Formula	C₁₉H₁₆ClNO₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	53-86-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Indometacin,NSC-77541			Smiles	CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)O

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	[1] https://pubmed.ncbi.nlm.nih.gov/11313997/ [2] https://pubmed.ncbi.nlm.nih.gov/16282546/ [3] https://pubmed.ncbi.nlm.nih.gov/7906675/ [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 2024-05-22)

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	--

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Indomethacin COX inhibitor

Chemical Structure

Molecular Weight: 357.79