product name Teriflunomide
Description: Teriflunomide, aslo known as A77 1726, is the active metabolite of leflunomide, which inhibits pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, and is used as an immunomodulatory agent for the treatment of arthritis and as an emerging oral therapy for multiple sclerosis (MS). Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS.
References: Ther Clin Risk Manag. 2013;9:177-90.
270.21
Formula
C12H9F3N2O2
CAS No.
108605-62-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 32 mg/mL (118.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
A77 1726, HMR-1726
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19410510
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
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| References | Ther Clin Risk Manag. 2013;9:177-90. |
