A77 1726 |  | | SYNONYMS | N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide
2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide | | | | PRODUCT LINE | Signal Transduction | | | | PRODUCT FAMILIES | Tyrosine Kinase Inhibitors | | | | | Ordering Information | | | Product Numbers | Format | Size | Unit Price | Quantity | | | ALX-430-096-M005 |
|
5 mg | | | | | ALX-430-096-M025 |
|
25 mg | | | | | | |
| | | Product Specification | | |
| FORMULA: | C12H9F3N2O2 | | | | | |
| MW: | 270.2 | | | | | |
| CAS NUMBER: | 108605-62-5 | | | | | |
| PURITY: | ≥98% | | | | | |
| APPEARANCE: | White solid. | | | | | |
| SOLUBILITY: | Soluble in DMSO. | | | | | |
| SHIPPING: | AMBIENT | | | | | |
| LONG TERM STORAGE: | +4°C | | | | | |
| HANDLING: | Protect from light. Keep under inert gas. | | | | | | Product Description | Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No. ALX-430-095). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2) in vitro and in vivo. |
| | | Product Specific Literature References | Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Full Text; http://www.jbc.org/cgi/reprint/270/21/12398
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms: R.T. Elder, et al.; J. Immunol. 159, 22 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression: S.K. Manna & B.B. Aggarwal; J. Immunol. 162, 2095 (1999) Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999) Abstract |
| | | | | RELATED PRODUCT GROUPS | Immunology > Immunomodulators > Immunomodulators Other Products / Signal Transduction > NF-kB Pathway > NF-kB Pathway Inhibitors / Inflammation > Cyclooxygenases [COX] / Related Products > COX Inhibitors | | | | | |
