Teriflunomide
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.
Purity & Quality Control
Choose Selective Dehydrogenase Inhibitors
Biological Activity
| Description | Teriflunomide 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. | 108605-62-5 |
| Storage | powder |
| in solvent | |
| Synonyms | A77 1726, HMR-1726 |
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 (g) = Concentration (mol/L) × Volume (L) × 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 MSDS / 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 MSDS / COA (available online).
Molecular Weight Calculator
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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 | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03526224 | Active not recruiting | Tecfidera|Teriflunomide | University at Buffalo | June 4 2018 | -- |
| NCT02425644 | Active not recruiting | Multiple Sclerosis | Actelion | June 4 2015 | Phase 3 |
| NCT02792231 | Recruiting | Relapsing Multiple Scelrosis | Novartis Pharmaceuticals|Novartis | August 26 2016 | Phase 3 |
| NCT03122652 | Recruiting | Multiple Sclerosis | Centre Hospitalier Universitaire de Nice|Genzyme a Sanofi Company | September 25 2017 | Phase 3 |
| NCT03198351 | Recruiting | Multiple Sclerosis | Sanofi | April 25 2013 | -- |
| NCT02833714 | Terminated | RELAPSING REMITTING MULTIPLE SCLEROSIS | University of North Carolina Chapel Hill|Genzyme a Sanofi Company | January 2016 | -- |
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.
