Leflunomide

Catalog No.S1247 Synonyms: HWA486

Leflunomide Chemical Structure

Molecular Weight(MW): 270.21

Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.

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In DMSO USD 190 In stock
USD 147 In stock
USD 470 In stock
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3 Customer Reviews

  • 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.

  • 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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Biological Activity

Description Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.
Targets
Dihydroorotate dehydrogenase [1]
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]

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)
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
Formula

C12H9F3N2O2

CAS No. 75706-12-6
Storage powder
Synonyms HWA486

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID