Teriflunomide
For research use only.
Catalog No.S4169 Synonyms: A77 1726, HMR-1726
13 publications
CAS No. 163451-81-8, 108605-62-5
Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.
Purity & Quality Control
Choose Selective Dehydrogenase Inhibitors
Biological Activity
| Description | Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent. | |
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| Targets |
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| In vitro |
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. [1] |
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| 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. [1] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 32 mg/mL (118.42 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | ',1 mg/mL |
* 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.
Chemical Information
| Molecular Weight | 270.21 |
|---|---|
| Formula | C12H9F3N2O2 |
| CAS No. | 163451-81-8, 108605-62-5 |
| Storage |
powder in solvent |
| Synonyms | A77 1726, HMR-1726 |
| Smiles | CC(=C(C#N)C(=O)NC1=CC=C(C=C1)C(F)(F)F)O |
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 | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
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 μL 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.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
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 SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04799288 | Not yet recruiting | Drug: Teriflunomide | HAM/TSP | National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC) | September 7 2021 | Phase 1|Phase 2 |
| NCT04129736 | Recruiting | Drug: Teriflunomide 14 MG | Multiple Sclerosis Pharmacokinetics | Jan Lycke|Sahlgrenska University Hospital Sweden | October 10 2019 | Phase 4 |
| NCT03526224 | Completed | Drug: Dimethyl Fumarate|Drug: Teriflunomide | Tecfidera|Teriflunomide | University at Buffalo | June 14 2018 | -- |
| NCT03561402 | Completed | 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 | -- |
Tech Support
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
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Question 1:
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?
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Answer:
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.
