Biological Activity
Inhibitor of dihydroorotate dehydrogenase (Kd = 12 nM; Ki = 179 nM). Inhibits proliferation of mitogen- or cytokine-stimulated lymphoid cells in vitro by inhibiting cell cycle progression from G1 to S. Imunosuppressive agent. Active metabolite of leflunomide (Cat. No. 2228).
Compound Libraries
Teriflunomide is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 270.21 |
| Formula | C12H9F3N2O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 108605-62-5 |
| PubChem ID | 54684141 |
| InChI Key | UTNUDOFZCWSZMS-YFHOEESVSA-N |
| Smiles | O=C(/C(C#N)=C(O)/C)NC1=CC=C(C(F)(F)F)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.02 | 100 | |
| ethanol | 1.35 | 5mM with sonication |
Preparing Stock Solutions
The following data is based on the product molecular weight 270.21. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.7 mL | 18.5 mL | 37.01 mL |
| 5 mM | 0.74 mL | 3.7 mL | 7.4 mL |
| 10 mM | 0.37 mL | 1.85 mL | 3.7 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.74 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Williamson et al (1995) Dihydroorotate dehydrogenase is a high affinity binding protein for A77 1726 and mediator of a range of biological effects of the immunomodulatory compound. J.Biol.Chem. 270 22467 PMID: 7673235
Davis et al (1996) The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry 35 1270 PMID: 8573583
Iglesias-Bregna et al (2013) Effects of prophylactic and therapeutic teriflunomide in transcranial magnetic stimulation-induced motor-evoked potentials in the dark agouti rat model of experimental autoimmune encephalomyelitis. J.Pharmacol.Exp.Ther. 347 203 PMID: 23892570
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