Teriflunomide (Synonyms: A77 1726)

Name: Teriflunomide
Brand: MedChemExpress
SKU: HY-15405
Rating: 5.0 (14 reviews)

Cat. No.: HY-15405 Purity: 99.92%: Data Sheet
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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.

CAS No. : 163451-81-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Teriflunomide:

Teriflunomide-d₄ In-stock
Teriflunomide (Standard) Get quote

14 Publications Citing Use of MCE Teriflunomide

Cell Proliferation/Viability Assay

Histological Imaging/Staining

2D/3D Cell Culture and Differentiation

: 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.

: 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.

: Teriflunomide purchased from MedChemExpress. Usage Cited in: Vet Sci. 2023 Aug 9;10(8):513.; 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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Biological Activity
Purity & Documentation
References
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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

Molecular Weight

270.21

Formula

C₁₂H₉F₃N₂O₂

CAS No.

163451-81-8

Appearance

Solid

Color

White to off-white

SMILES

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.92%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (246 KB) RP-HPLC (261 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]

Complete Stock Solution Preparation Table

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

Teriflunomide Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Teriflunomide163451-81-8A77 1726Drug MetaboliteInhibitorinhibitorinhibit

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Teriflunomide (Synonyms: A77 1726)

Customer Review

Other Forms of Teriflunomide:

Teriflunomide Related Antibodies

14 Publications Citing Use of MCE Teriflunomide

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Biological Activity

Purity & Documentation

References

Customer Review

Teriflunomide Related Antibodies

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Complete Stock Solution Preparation Table

Teriflunomide Related Classifications

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