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 Details
| Alternative Name: | N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide |
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| Formula: | C12H9F3N2O2 |
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| MW: | 270.2 |
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| CAS: | 108605-62-5 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Determined by NMR. |
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| Appearance: | White solid. |
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| Solubility: | Soluble in DMSO. |
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| Shipping: | Ambient |
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| Long Term Storage: | +4°C |
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| Handling: | Protect from light. Keep under inert gas. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Mitochondrial dysfunction induced by leflunomide and its active metabolite: J. Xuan, et al.; Toxicology
396, 33 (2018),
Abstract;
Full Text
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;
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;
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;
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;
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;
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem.
270, 12398 (1995),
Abstract;
Full Text
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett.
334, 161 (1993),
Abstract;
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