For research use only.
Catalog No.S4169 Synonyms: A77 1726, HMR-1726
Molecular Weight(MW): 270.21
Teriflunomide is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.
Selleck's Teriflunomide has been cited by 5 publications
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|Description||Teriflunomide is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.|
Teriflunomide primarily acts as an inhibitor of dihydroorotate dehydrogenase (DHODH), a key mitochondrial enzyme involved in the de novo synthesis of pyrimidines in rapidly proliferating cells. By reducing the activity of high-avidity proliferating T lymphocytes and B lymphocytes, teriflunomide likely attenuates the inflammatory response to autoantigens in MS. Thus, teriflunomide can be considered a cytostatic rather than a cytotoxic drug to leukocytes. 
|In vivo||Teriflunomide has demonstrated beneficial effects in two independent animal models of demyelinating disease. In the dark agouti rat model of experimental autoimmune encephalitis (EAE), teriflunomide administration results in clinical, histopathological, and electrophysiological evidence of efficacy both as a prophylactic and therapeutic agent. Similarly, in the female Lewis rat model of EAE, teriflunomide administration results in beneficial prophylactic and therapeutic clinical effects, with a delay in disease onset and symptom severity. |
|In vitro||DMSO||32 mg/mL (118.42 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||A77 1726, HMR-1726|
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||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* 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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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04129736||Recruiting||Drug: Teriflunomide 14 MG||Multiple Sclerosis Pharmacokinetics||Jan Lycke|Sahlgrenska University Hospital Sweden||October 10 2019||Phase 4|
|NCT03526224||Active not recruiting||Drug: Dimethyl Fumarate|Drug: Teriflunomide||Tecfidera|Teriflunomide||University at Buffalo||June 4 2018||--|
|NCT03561402||Recruiting||Drug: Teriflunomide||Multiple Sclerosis Relapsing-Remitting||McGill University||December 1 2016||--|
|NCT02833714||Terminated||--||RELAPSING REMITTING MULTIPLE SCLEROSIS||University of North Carolina Chapel Hill|Genzyme a Sanofi Company||January 2016||--|
|NCT02679885||Completed||--||Multiple Sclerosis||Griffin Hospital||October 2015||--|
|NCT02263547||Terminated||Drug: teriflunomide|Drug: Colestipol||Teriflunomide Elimination|Healthy Volunteers||Derrick Scott Robertson|Genzyme a Sanofi Company|University of South Florida||March 2015||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
I am planning to use teriflunomide (S4169) in my in vivo protocol, but I cannot get a homogeneous solution. Could you please provide me with some guidance?
This compound is an oral clinical medicine. For oral administration suspension is fine. In paper http://www.pnas.org/content/108/44/18067.full, they also prepared the stock by DMSO and then diluted into 0.9% sterile saline for animial study.