Home Metabolism Dehydrogenase inhibitor - Immunology & Inflammation related chemical Teriflunomide

Teriflunomide

Catalog No.S4169 Synonyms: A77 1726, HMR-1726

For research use only.

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

CAS No. 163451-81-8

Selleck's Teriflunomide has been cited by 17 publications

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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

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 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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 270.21
Formula

C12H9F3N2O2
CAS No. 163451-81-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=C(C#N)C(=O)NC1=CC=C(C=C1)C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

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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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04799288 Recruiting Drug: Teriflunomide 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 Recruiting Drug: Teriflunomide 14 MG Multiple Sclerosis Pharmacokinetics Jan Lycke|Sahlgrenska University Hospital Sweden October 10 2019 Phase 4
NCT03526224 Completed Drug: Dimethyl Fumarate|Drug: Teriflunomide Tecfidera|Teriflunomide University at Buffalo June 14 2018 --
NCT03561402 Completed Drug: Teriflunomide 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 --
NCT02679885 Completed -- Multiple Sclerosis Griffin Hospital October 2015 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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