Leflunomide (HWA486)
For research use only.
Catalog No.S1247 Synonyms: RS-34821, SU101, Arava
6 publications
CAS No. 75706-12-6
Leflunomide (HWA486, RS-34821, SU101, Arava) 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.
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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 (HWA486) 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 (HWA486) 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 (HWA486) purchased from Selleck.
H1299, H460, A549 cells were treated with leflunomide or teriflunomide at indicated concentrations for 24 h.
Toxicol Lett, 2018, . Leflunomide (HWA486) purchased from Selleck.
Purity & Quality Control
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Biological Activity
| Description | Leflunomide (HWA486, RS-34821, SU101, Arava) 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. | |||||||||||||||||||||||||||||||||||||
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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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| Water | Insoluble | |
| Ethanol | ''54 mg/mL |
* 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 | RS-34821, SU101, Arava |
| Smiles | CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
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| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
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Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
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 | Unknown status | Drug: Prednisone|Drug: Prednisone and Leflunomide | Autoimmune Disease | Peking Union Medical College Hospital | July 1 2018 | Not Applicable |
| NCT01611675 | Terminated | Drug: Vemurafenib|Drug: Leflunomide | Melanoma | Massachusetts General Hospital | July 2012 | Phase 1 |
| NCT00802243 | Unknown status | Drug: leflunomide | Bullous Pemphigoid | University Hospital Limoges | September 2007 | Phase 2 |
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