Leflunomide
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.
Cited by 2 Publications
3 Customer Reviews
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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.
Peritoneal macrophages were stained for FITC-MR. Flow cytometry analysis of MFI. The result for one representative of three independent experiments is shown.
Cell Immunol 2014 288(1-2), 1-7. Leflunomide purchased from Selleck.
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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.
Purity & Quality Control
Choose Selective Dehydrogenase Inhibitors
Biological Activity
| Description | Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent. | |
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| In vitro |
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. [1] 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. [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. [3] |
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| In vivo | Leflunomide is able to prevent and reverse allograft and xenograft rejection in rodents, dogs, and monkeys. [2] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 54 mg/mL (199.84 mM) |
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| Ethanol | 54 mg/mL (199.84 mM) | |
| Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 270.21 |
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| Formula | C12H9F3N2O2 |
| CAS No. | 75706-12-6 |
| Storage | powder |
| in solvent | |
| Synonyms | HWA486 |
Bio Calculators
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator
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 |
| NCT02703194 | Recruiting | Immunoglobulin G4 Related Sclerosing Disease | Chinese PLA General Hospital | March 2016 | Phase 4 |
| NCT02024334 | Unknown status | Juvenile Idiopathic Arthritis | Mashhad University of Medical Sciences | June 2013 | Phase 4 |
| NCT01749787 | Completed | Arthritis Rheumatoid | Protalex Inc. | November 2012 | Phase 1 |
| NCT01727193 | Recruiting | Myasthenia Gravis | First Affiliated Hospital Sun Yat-Sen University | September 2012 | Phase 3 |
| NCT01659242 | Terminated | Rheumatoid Arthritis | Singapore General Hospital | July 2012 | Phase 4 |
Tech Support
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