163451-81-8 factory in China A77 1726 factory in China 163451-81-8 seller in China
A77 1726 Basic information |
Product Name: | A77 1726 |
Synonyms: | A77 1726 (Teriflunomide);LeflunoMide EP IMpurity B;A 1726;Flucyamide;HMR 1726;(Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide |
CAS: | 163451-81-8 |
MF: | C12H9F3N2O2 |
MW: | 270.2072696 |
EINECS: | |
Product Categories: | Metabolites & Impurities;Tyrosine Kinase Inhibitors |
Mol File: | 163451-81-8.mol |
A77 1726 Chemical Properties |
Melting point | 229-232°C |
storage temp. | Hygroscopic, -20°C Freezer, Under Inert Atmosphere |
A77 1726 Usage And Synthesis |
Chemical Properties | White Solid |
Uses | The active metabolite of Leflunomide, a potent disease-modifying antirheumatic drug used in the treatment of rheumatoid arthritis. LEF-M interferes with dendritic cell function. |
Definition | ChEBI: An enamide obtained by formal condensation of the carboxy group of (2Z)-2-cyano-3-hydroxybut-2-enoic acid with the anilino group of 4-(trifluoromethyl)aniline. Used for the treatment of relapsing forms of multiple sclerosis and rheumatoid arthritis. |
Uses | A-771726 is the active metabolite of leflunomide, a prodrug approved by the FDA for treatment of rheumatoid arthritis. A-771726 reversibly inhibits dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines. It prevents activated lymphocytes from accumulating sufficient pyrimidines to support DNA synthesis (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively). At higher doses, A-771726 inhibits tyrosine kinases responsible for early T cell and B cell signaling in the G0/G1 phase of the cell cycle. A-771726 has also been shown to inhibit the production of prostaglandin E2 in synoviocytes activated by TNF-α and IL-1α (IC50s = 7 and 3 μM, respectively) as well as inhibit MMP-1 and IL-6 production at concentrations >10 μM.[Cayman Chemical] |
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