Teriflunomide
Based on 14 publication(s) in Google Scholar
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 163451-81-8
- Formula: C12H9F3N2O2
- Molecular Weight:270.21
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Teriflunomide
More- Cell Stem Cell. 2021 Nov 4;28(11):1982-1999.e8. [Abstract]
- Mol Cell. 2025 Dec 4;85(23):4347-4364.e12. [Abstract]
- Biomed Pharmacother. 2019 Oct:118:109305. [Abstract]
- Cell Rep. 2023 Aug 18;42(8):113016. [Abstract]
- J Med Chem. 2021 Sep 23;64(18):13918-13932. [Abstract]
- CNS Neurosci Ther. 2023 Jul;29(7):1923-1939. [Abstract]
- J Med Virol. 2025 Jul;97(7):e70488. [Abstract]
- J Med Virol. 2024 Jan;96(1):e29372. [Abstract]
- Mol Neurobiol. 2024 Apr;61(4):1936-1952. [Abstract]
- Antiviral Res. 2026 Mar:247:106354. [Abstract]
- Expert Rev Clin Immunol. 2019 Jul;15(7):801-808. [Abstract]
- ChemMedChem. 2024 Jun 18:e202400292. [Abstract]
- Vet Sci. 2023 Aug 9;10(8):513. [Abstract]
- Res Sq. 2025 Sep 14.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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2D/3D Cell Culture and Differentiation
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Histological Imaging/Staining
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WB
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IF
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
26.65 μM
Compound: 2, A-771726
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Cytotoxicity against human Jurkat cells after 4 days by MTT assay
Cytotoxicity against human Jurkat cells after 4 days by MTT assay
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[PMID: 22984987] |
| Jurkat | IC50 |
43.22 μM
Compound: A771726
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Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method
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[PMID: 28235702] |
| Jurkat | IC50 |
43.22 μM
Compound: Teriflunomide
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Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
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[PMID: 29939742] |
| Jurkat | IC50 |
60 μM
Compound: 25
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Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay
Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay
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[PMID: 26079043] |
| MDA-MB-231 | IC50 |
14 μM
Compound: Teriflunomide
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Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
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[PMID: 34516133] |
| MDA-MB-468 | IC50 |
>20 μM
Compound: Teriflunomide
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Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay
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[PMID: 34516133] |
| PBMC | IC50 |
46 μM
Compound: 3
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Antiproliferative activity against PHA-stimulated human PBMC assessed as inhibition of [3H]-thymidine incorporation after 72 hrs by BrdU-ELISA assay
Antiproliferative activity against PHA-stimulated human PBMC assessed as inhibition of [3H]-thymidine incorporation after 72 hrs by BrdU-ELISA assay
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[PMID: 22078215] |
| PBMC | IC50 |
54.3 μM
Compound: A771726
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Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by BrdU incorporation assay
Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by BrdU incorporation assay
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[PMID: 28235702] |
| Splenocyte | IC50 |
6.7 μM
Compound: A-771726
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Inhibition of Concanavalin A-stimulated cell proliferation in mouse splenocytes after 48 hrs by MTT assay
Inhibition of Concanavalin A-stimulated cell proliferation in mouse splenocytes after 48 hrs by MTT assay
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[PMID: 11000020] |
| T-cell | IC50 |
48.03 μM
Compound: 2, A-771726
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Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay
Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay
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[PMID: 22984987] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 163451-81-8
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Appearance Solid
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Molecular Weight 270.21
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Formula C12H9F3N2O2
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Color White to off-white
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SMILES
C/C(O)=C(C(NC1=CC=C(C=C1)C(F)(F)F)=O)\C#N
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Synonyms
A77 1726
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (14)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
Aspartate availability limits hematopoietic stem cell function during hematopoietic regeneration. [Abstract]2021 Nov 4;28(11):1982-1999.e8. PMID: 34450065 -
Mol Cell
2025 Dec 4;85(23):4347-4364.e12. PMID: 41270758 -
Biomed Pharmacother
Antiviral effects of selected IMPDH and DHODH inhibitors against foot and mouth disease virus. [Abstract]2019 Oct:118:109305. PMID: 31545264 -
Cell Rep
Neuroendocrine lineage commitment of small cell lung cancers can be leveraged into p53-independent non-cytotoxic therapy. [Abstract]2023 Aug 18;42(8):113016. PMID: 37597186
Teriflunomide purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Aug 18;42(8):113016. [Abstract]
Teriflunomide 10 μM decreased proliferation of SCLC cells F1339, H82, and H146.
Teriflunomide purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Aug 18;42(8):113016. [Abstract]
Teriflunomide (10 μM) treatment induced morphology changes of terminal differentiation, e.g., decrease in nuclear/cytoplasmic ratio.
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J Med Chem
Exploring Marine-Derived Ascochlorins as Novel Human Dihydroorotate Dehydrogenase Inhibitors for Treatment of Triple-Negative Breast Cancer. [Abstract]2021 Sep 23;64(18):13918-13932. PMID: 34516133 -
CNS Neurosci Ther
Dihydroorotate dehydrogenase regulates ferroptosis in neurons after spinal cord injury via the P53-ALOX15 signaling pathway. [Abstract]2023 Jul;29(7):1923-1939. PMID: 36942513
Teriflunomide purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2023 Jul;29(7):1923-1939. [Abstract]
HE staining showed that inflammatory response and tissue damage of SCI + Teriflunomide (10 mg/kg) group were significantly heavier than other groups after spinal cord injury. In this group, inflammatory cells and tissue edema increased.
Teriflunomide purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2023 Jul;29(7):1923-1939. [Abstract]
Western Blot results showed that ACSL4 and COX2 expression were significantly increased in SCI + Teriflunomide (10 mg/kg) group compared with the other three groups.
Teriflunomide purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2023 Jul;29(7):1923-1939. [Abstract]
Immunofluorescence showed that the expression of GPX4 in spinal cord neurons of the other three groups was significantly increased compared with SCI + Teriflunomide (10 mg/kg)-treated spinal cord neurons.
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J Med Virol
In Vitro Synergistic Antiviral Effects of β-D-N4-hydroxycytidine and Teriflunomide in Combination against a Broad Range of RNA Viruses. [Abstract]2025 Jul;97(7):e70488. PMID: 40600448 -
J Med Virol
Identification of dihydroorotate dehydrogenase inhibitor, vidofludimus, as a potent and novel inhibitor for influenza virus. [Abstract]2024 Jan;96(1):e29372. PMID: 38235544 -
Mol Neurobiol
Teriflunomide Promotes Blood-Brain Barrier Integrity by Upregulating Claudin-1 via the Wnt/β-catenin Signaling Pathway in Multiple Sclerosis. [Abstract]2024 Apr;61(4):1936-1952. PMID: 37819429 -
Antiviral Res
Lapachol, a dihydroorotate dehydrogenase inhibitor, demonstrates antiviral activity against feline calicivirus in vitro and in vivo. [Abstract]2026 Mar:247:106354. PMID: 41577199 -
Expert Rev Clin Immunol
Additive immunosuppressive effect of leflunomide and hydroxychloroquine supports rationale for combination therapy for Sjögren's syndrome. [Abstract]2019 Jul;15(7):801-808. PMID: 31192747 -
ChemMedChem
Synthesis and Characterization of DHODH Inhibitors Based on the Vidofludimus Scaffold with Pronounced Anti-SARS-CoV-2 Activity. [Abstract]2024 Jun 18:e202400292. PMID: 38887198 -
Vet Sci
Comparative Evaluation of GS-441524, Teriflunomide, Ruxolitinib, Molnupiravir, Ritonavir, and Nirmatrelvir for In Vitro Antiviral Activity against Feline Infectious Peritonitis Virus. [Abstract]2023 Aug 9;10(8):513. PMID: 37624300
Teriflunomide purchased from MedChemExpress. Usage Cited in: Vet Sci. 2023 Aug 9;10(8):513. [Abstract]
The CC50, EC50, and SI for six compounds against FIPV. The half-maximal cytotoxic concentration (CC50) values are from four measurements of diluted drugs using MTT assay, in CRFK cells treated with drugs for 48 h. The half-maximal effective concentration (EC50) values are from six measurements of diluted drugs against FIPV replication in CRFK cells for 48 h. Based on the SI value (mean CC50)/(mean EC50), GS-441524 was found highly selective (SI 165.5) against FIPV among the drugs tested and showed high efficacy (EC50 1.6 µM) against FIPV with a less deleterious effect (CC50 260.0 µM) on the cells. Nirmatrelvir also showed promising efficacy (EC50 2.5 µM) and selectivity (SI 113.7) against FIPV. Ritonavir showed the highest toxicity level in the cells (CC50 39.9).
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Solvent & Solubility
DMSO : 33.33 mg/mL (123.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.25 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7008 mL | 18.5041 mL | 37.0083 mL | 92.5206 mL |
| 5 mM | 0.7402 mL | 3.7008 mL | 7.4017 mL | 18.5041 mL | |
| 10 mM | 0.3701 mL | 1.8504 mL | 3.7008 mL | 9.2521 mL | |
| 15 mM | 0.2467 mL | 1.2336 mL | 2.4672 mL | 6.1680 mL | |
| 20 mM | 0.1850 mL | 0.9252 mL | 1.8504 mL | 4.6260 mL | |
| 25 mM | 0.1480 mL | 0.7402 mL | 1.4803 mL | 3.7008 mL | |
| 30 mM | 0.1234 mL | 0.6168 mL | 1.2336 mL | 3.0840 mL | |
| 40 mM | 0.0925 mL | 0.4626 mL | 0.9252 mL | 2.3130 mL | |
| 50 mM | 0.0740 mL | 0.3701 mL | 0.7402 mL | 1.8504 mL | |
| 60 mM | 0.0617 mL | 0.3084 mL | 0.6168 mL | 1.5420 mL | |
| 80 mM | 0.0463 mL | 0.2313 mL | 0.4626 mL | 1.1565 mL | |
| 100 mM | 0.0370 mL | 0.1850 mL | 0.3701 mL | 0.9252 mL |
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