Home Metabolism Dehydrogenase inhibitor - Immunology & Inflammation related chemical Teriflunomide For research use only.

Teriflunomide

Synonyms: A77 1726, HMR-1726

Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.

Teriflunomide Chemical Structure

Teriflunomide Chemical Structure

CAS No. 163451-81-8

Purity & Quality Control

Teriflunomide Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Biological Activity

Description Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.
Targets
dihydroorotate dehydrogenase [1]
In vitro
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]
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04799288 Recruiting
HAM/TSP
National Institute of Neurological Disorders and Stroke (NINDS)|National Institutes of Health Clinical Center (CC)
 September 24 2021 Phase 1|Phase 2
NCT04129736 Completed
Multiple Sclerosis Pharmacokinetics
Jan Lycke|Sahlgrenska University Hospital Sweden
 October 10 2019 Phase 4
NCT03526224 Completed
Tecfidera|Teriflunomide
University at Buffalo
 June 14 2018 --
NCT03561402 Completed
Multiple Sclerosis Relapsing-Remitting
McGill University
 December 1 2016 --
NCT02833714 Terminated
RELAPSING REMITTING MULTIPLE SCLEROSIS
University of North Carolina Chapel Hill|Genzyme a Sanofi Company
 January 2016 --

Chemical Information & Solubility

Molecular Weight 270.21 Formula

C12H9F3N2O2
CAS No. 163451-81-8 SDF Download Teriflunomide SDF
Smiles CC(=C(C#N)C(=O)NC1=CC=C(C=C1)C(F)(F)F)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 27 mg/mL ( (99.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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.

Handling Instructions

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Frequently Asked Questions

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?

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.

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