For research use only.
Catalog No.S1247 Synonyms: HWA486
CAS No. 75706-12-6
Leflunomide (HWA486) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.
Selleck's Leflunomide has been cited by 6 publications
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Peritoneal macrophages were pretreated for 1 h with the leﬂunomide (100 umol/L), followed by treatment with 10 ug/ml rTsP53 for 6 h. Western blot analysis of P-STAT6 and STAT6 expression was performed. Corresponding staining for b-actin was carried out to control for equal loading. *P < 0.05 versus control group, #P < 0.05 versus rTsP53 group.
Cell Immunol 2014 288(1-2), 1-7. Leflunomide purchased from Selleck.
We found that the expression of Arg1, Ym1 and IL-10 on peritoneal macrophages incubated with leflunomide and rTsP53 were significantly down-regulated in comparison to treatment with rTsP53 alone.
Cell Immunol 2014 288(1-2), 1-7. Leflunomide purchased from Selleck.
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|Description||Leflunomide (HWA486) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.|
Leflunomide is actually a prodrug that is processed in vivo to the active metabolite A771726，which has been shown to inhibit proliferation of mononuclear and T-cells. Leflunomide is an inhibitor of several protein tyrosine kinases, with IC50 values between 30 mM and 100 mM in vitro cellular and enzymatic assays.  Leflunomide is capable of inhibiting anti-CD3- and interleukin-2 (IL-2)-stimulated T cell proliferation. Leflunomide is able to inhibit p59fyn and p56lck activity in in vitro tyrosine kinase assays. Leflunomide also inhibits Ca2+ mobilization in Jurkat cells stimulated by anti-CD3 antibody but not in those stimulated by ionomycin. Leflunomide also inhibits distal events of anti-CD3 monoclonal antibody stimulation, namely, IL-2 production and IL-2 receptor expression on human T lymphocytes. Leflunomide also inhibits tyrosine phosphorylation in CTLL-4 cells stimulated by IL-2.  Leflunomide is an immunomodulatory drug that may exert its effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which plays a key role in the de novo synthesis of the pyrimidine ribonucleotide uridine monophosphate (rUMP). Leflunomide prevents the expansion of activated and autoimmune lymphocytes by interfering with the cell cycle progression due to inadequate production of rUMP and utilizing mechanisms involving p53. 
|In vivo||Leflunomide is able to prevent and reverse allograft and xenograft rejection in rodents, dogs, and monkeys. |
|In vitro||DMSO||54 mg/mL (199.84 mM)|
|Ethanol||54 mg/mL (199.84 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04212416||Recruiting||Drug: Leflunomide||Chronic Graft Versus Host Disease|Steroid Refractory Graft Versus Host Disease||City of Hope Medical Center|National Cancer Institute (NCI)||May 12 2020||Phase 1|
|NCT04361214||Recruiting||Drug: Leflunomide||COVID-19||University of Chicago||May 5 2020||Phase 1|
|NCT03715699||Recruiting||Drug: Prednisone|Drug: Prednisone and Leflunomide||Autoimmune Disease||Peking Union Medical College Hospital||July 1 2018||Not Applicable|
|NCT03599986||Completed||--||Active Rheumatoid Arthritis||Eva Pharma|DataClin||June 16 2017||--|
|NCT01500551||Recruiting||Drug: Tofacitinib||Juvenile Idiopathic Arthritis||Pfizer||March 18 2013||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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