Catalog No.S1247 Synonyms: HWA486
Molecular Weight(MW): 270.21
Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.
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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.
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|Description||Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.|
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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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00101374||Completed||HIV Infections||National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC)||January 5, 2005||Phase 1|
|NCT02981979||Not yet recruiting||Takayasu Arteritis||Jiang lindi|Shanghai Zhongshan Hospital||December 2016||--|
|NCT02930343||Recruiting||Rheumatoid Arthritis||Jawaharlal Institute of Postgraduate Medical Education & Research||September 2016||Phase 4|
|NCT02703194||Recruiting||Immunoglobulin G4 Related Sclerosing Disease||Chinese PLA General Hospital||March 2016||Phase 4|
|NCT02878161||Enrolling by invitation||Rheumatoid Arthritis||Fen Li|Central South University||January 2016||Phase 4|
|NCT02644499||Active, not recruiting||Rheumatoid Arthritis||Jawaharlal Institute of Postgraduate Medical Education & Research||December 2015||Phase 4|
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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