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| 1g |
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| Other Sizes |
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| ln Vitro |
In vitro antitumor activity of indomethacin sodium hydrate (0-150 μM; 24 hours; 3LL-D122 cells) has been shown [2]. By activating PKR and phosphorylating eLF2α, indomethacin sodium hydrate (0-1000 μM) inhibits viral replication (IC50=2 μM) and stops viral protein translation, protecting host cells from viral harm [3]. NaCl indomethacin hydrate
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| ln Vivo |
Carrageenan-induced hyperalgesia is dose-dependently reversed by indomethacin (Indometacin) sodium hydrate (0.01-10 mg/kg; oral; 3 hours; male Sprague-Dawley rats) which also causes paw edema and hyperalgesia [1]. Tumor growth is inhibited in vivo by indomethacin (10 mg/mL; oral; once daily for 29 days; male C57BL/6J mice) [2].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: 3LL-D122 cells (highly metastatic variant of mouse LLcarcinoma cells) Tested Concentrations: 0, 20, 50, 100 and 150μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited cell viability at 20 mM, with 50% inhibition at 60 mM. Cell Cycle Analysis[2] Cell Types: 3LL-D122 cells (highly metastatic variant of mouse LLcarcinoma cells) Tested Concentrations: 0, 30 and 80μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished in the percentage of cells at the G2/M phase and increased in the percentage of cells at G1 phase. |
| 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. |
| Molecular Formula |
C19H21CLNNAO7
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|---|---|
| Molecular Weight |
433.82
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| CAS # |
74252-25-8
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| Related CAS # |
Indomethacin;53-86-1;Indomethacin-d4;87377-08-0;Indomethacin;53-86-1;Indomethacin sodium;7681-54-1
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| SMILES |
O.O.O.[Na+].COC1C=CC2N(C(=C(CC([O-])=O)C=2C=1)C)C(C1C=CC(Cl)=CC=1)=O
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| Solubility (In Vitro) |
H2O : 25 mg/mL (57.63 mM)
DMSO : 12.5 mg/mL (28.81 mM ) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.79 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 (4.79 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: 5 mg/mL (11.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3051 mL | 11.5255 mL | 23.0510 mL | |
| 5 mM | 0.4610 mL | 2.3051 mL | 4.6102 mL | |
| 10 mM | 0.2305 mL | 1.1526 mL | 2.3051 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.
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