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Purity: ≥98%
Indomethacin (Indometacin; Indocin) is a potent and non-selective COX1 and COX2 inhibitor of the nonsteroidal anti-inflammatory drug (NSAID) class with an IC50 of 0.1 μg/mL and 5 μg/mL, respectively. Indomethacin is a synthetic nonsteroidal indole derivative with anti-inflammatory activity and chemopreventive properties and is used to reduce fever, pain, stiffness, and swelling. Indomethacin inhibits the enzyme cyclooxygenase, thereby preventing cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines.
ln Vitro |
In vitro antitumor activity of indomethacin (Indometacin) (0-150 μM; 24 hours; 3LL-D122 cells) has been reported [2]. By activating PKR and phosphorylating eF2α, indomethacin (Indometacin) (0-1000 μM) inhibits viral replication (IC50=2 μM) and stops viral protein translation, protecting host cells from viral harm [3]. M1 type RAW 264.7 cells undergo M2 type differentiation when exposed to 8 μM of indomethacin for 26 hours [4]. Human adipose-derived stem cells undergo transdifferentiation into neurogenic-like cells when exposed to indomethacin (200 μM) for five days [5].
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ln Vivo |
Using indomethacin, models of gastrointestinal ulcers can be created in animals.
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Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats[1]
Doses: 0.01-10 mg/kg Route of Administration: Oral administration; for 3 hrs (hours) Experimental Results: Inhibited the carrageenan-induced rat paw oedema (ED50=2.0 mg/kg) and hyperalgesia (ED50= 1.5 mg/kg) in a dose-dependent manner. Animal/Disease Models: Male C57BL/6J mice[2] Doses: 10 mg/mL Route of Administration: Oral administration; daily, for 29 days Experimental Results: Delayed the onset of tumor growth and the initial growth rate of the footpad tumors. |
References |
[1]. Riendeau D, et, al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.
[2]. Eli Y, et, al. Comparative effects of indomethacin on cell proliferation and cell cycle progression in tumor cells grown in vitro and in vivo. Biochem Pharmacol. 2001 Mar 1;61(5):565-71. [3]. Amici C, et, al. Inhibition of viral protein translation by indomethacin in vesicular stomatitis virus infection: role of eIF2α kinase PKR. Cell Microbiol. 2015 Sep;17(9):1391-404. [4]. Luo X, Xiong H, Jiang Y, et al. Macrophage Reprogramming via Targeted ROS Scavenging and COX-2 Downregulation for Alleviating Inflammation. Bioconjug Chem. 2023;34(7):1316-1326. [5]. Kompisch KM, Lange C, Steinemann D, et al. Neurogenic transdifferentiation of human adipose-derived stem cells? A critical protocol reevaluation with special emphasis on cell proliferation and cell cycle alterations. Histochem Cell Biol. 2010;134(5):453-468. |
Molecular Formula |
C19H16CLNO4
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Molecular Weight |
357.79
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CAS # |
53-86-1
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Related CAS # |
Indomethacin;53-86-1;Indomethacin sodium hydrate;74252-25-8
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SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C(N1C(C([H])([H])[H])=C(C([H])([H])C(=O)O[H])C2C([H])=C(C([H])=C([H])C1=2)OC([H])([H])[H])=O
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InChi Key |
CGIGDMFJXJATDK-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H16ClNO4/c1-11-15(10-18(22)23)16-9-14(25-2)7-8-17(16)21(11)19(24)12-3-5-13(20)6-4-12/h3-9H,10H2,1-2H3,(H,22,23)
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Chemical Name |
2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetic acid
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 1.25 mg/mL (3.49 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 1.25 mg/mL (3.49 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 1.25 mg/mL (3.49 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7949 mL | 13.9747 mL | 27.9494 mL | |
5 mM | 0.5590 mL | 2.7949 mL | 5.5899 mL | |
10 mM | 0.2795 mL | 1.3975 mL | 2.7949 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effect of DFU, indomethacin, piroxicam and DuP 697 on the production of PGE2 by arachidonic acid stimulated CHO cells stably transfected with human (a) COX-1 or (b) COX-2. Cells were preincubated for 15 min with indomethacin (♦), DuP 697 (•), piroxicam (▴) or DFU (▪) before stimulation with (a) 0.5 μm (COX-1) or (b) 10 μm (COX-2) arachidonic acid. td> |
Time-dependent inhibition of purified recombinant human COX-2 by DFU. (a) The enzyme was preincubated for different periods of time without (•), or with 12.5 μm (▪) or 100 μm (▴) DFU before initiation of the reaction with arachidonic acid. (b) Increase in the observed first order rate constant (kobs) for the formation of the tight enzyme-DFU complex as function of inhibitor concentration. td> |
Determination of inhibitor stoichiometry of purified COX-2 with DFU. Aliquots of COX-2 were preincubated with the inhibitor for 15 min before measurement of the cyclo-oxygenase reaction. The concentration of COX-2 (subunit) was 3.4 μm. td> |