Cat. No.: HY-15405

Teriflunomide

(Synonyms: A77 1726)

14 Cited Publications

Customer Review

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

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Teriflunomide Chemical Structure

CAS No.: 163451-81-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC₅₀	26.65 μM Compound: 2, A-771726	Cytotoxicity against human Jurkat cells after 4 days by MTT assay Cytotoxicity against human Jurkat cells after 4 days by MTT assay	[PMID: 22984987]
Jurkat	IC₅₀	43.22 μM Compound: A771726	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	[PMID: 28235702]
Jurkat	IC₅₀	43.22 μM Compound: Teriflunomide	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	[PMID: 29939742]
Jurkat	IC₅₀	60 μM Compound: 25	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	[PMID: 26079043]
MDA-MB-231	IC₅₀	14 μM Compound: Teriflunomide	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	[PMID: 34516133]
MDA-MB-468	IC₅₀	>20 μM Compound: Teriflunomide	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	[PMID: 34516133]
PBMC	IC₅₀	46 μM Compound: 3	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	[PMID: 22078215]
PBMC	IC₅₀	54.3 μM Compound: A771726	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	[PMID: 28235702]
Splenocyte	IC₅₀	6.7 μM Compound: A-771726	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	[PMID: 11000020]
T-cell	IC₅₀	48.03 μM Compound: 2, A-771726	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	[PMID: 22984987]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 163451-81-8
Appearance Solid
Molecular Weight 270.21
Formula C₁₂H₉F₃N₂O₂
Color White to off-white
SMILES

C/C(O)=C(C(NC1=CC=C(C=C1)C(F)(F)F)=O)\C#N
Synonyms

A77 1726
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (14)

All Cell Proliferation/Viability AssayHistological Imaging/Staining2D/3D Cell Culture and DifferentiationWBIF

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Journal Impact Factor

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

UMP functions as an endogenous regulator of NR4A1 to control gastric cancer progression. [Abstract]

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.
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.
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).
Res Sq

2025 Sep 14.

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.7008 mL

18.5041 mL

37.0083 mL

5 mM

0.7402 mL

3.7008 mL

7.4017 mL

10 mM

0.3701 mL

1.8504 mL

3.7008 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

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Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Oh J, et al. An update of teriflunomide for treatment of multiple sclerosis. Ther Clin Risk Manag. 2013;9:177-90. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Teriflunomide

14 Cited Publications

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Teriflunomide

Immunology/Inflammation Compound Library

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Publications Citing Use of MedChemExpress (MCE) Teriflunomide

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Teriflunomide

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Drug Metabolite Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Non-steroidal Anti-Inflammatory Compound Library

Off-patent Drug Library

Mitochondrial Toxicity Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Teriflunomide

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Teriflunomide Related Classifications

Cat. No.: HY-15405