A77 1726 CAS NO.163451-81-8

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

Safety Information

Hazard Codes	Xn
Risk Statements	22

MSDS Information

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]