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Indometacin Farnesil

Catalog No.GD15273 Copy One-Click Copy Product Info

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Indometacin Farnesil Chemical Structure

Cas No.: 85801-02-1

Size Price Stock Qty
25mg
$49.00
In stock
50mg
$80.00
In stock
100mg
$113.00
In stock
250mg
$226.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of Indometacin Farnesil

Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.

Indometacin farnesil (IMF) is a newly synthesized prodrug of indomethacin designed to reduce the occurrence of side-effects by esterification of the carboxyl group of indomethacin with farnesol. This modification is intended to decrease the extraction and subsequent rapid metabolism of the drug by the liver, so that lymphatic absorption would become a major route, and it was also anticipates that hydrolytic enzymes present in plasma and tissues, including inflamed tissue, would release indomethacin effectively from IMF[2].

Indomethacin farnesil (IMF) can effectively release indomethacin when administered locally[1].

[1]. S Kumakura, et al. Inhibitory effect of indomethacin farnesil, a novel antiinflammatory prodrug, on carrageenin-induced inflammation in rats. Agents Actions. 1990 Mar;29(3-4):286-91. 

[2]. M Mishima, et al. Metabolic fate of indometacin farnesil, a prodrug of indomethacin: characteristic biotransformation of indometacin farnesil in rats. Xenobiotica. 1990 Feb;20(2):135-46. 

[3]. 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. 

[4]. Jorge Vallecillo-Hern谩ndez, et al. Indomethacin Disrupts Autophagic Flux by Inducing Lysosomal Dysfunction in Gastric Cancer Cells and Increases Their Sensitivity to Cytotoxic Drugs. Sci Rep. 2018 Feb 26;8(1):3593. 

Chemical Properties of Indometacin Farnesil

Cas No. 85801-02-1 SDF
Formula M.Wt
Solubility Storage
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.
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**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

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In vivo Formulation Calculator (Clear solution) of Indometacin Farnesil

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

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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 % saline
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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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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